Category: 1334177-86-4

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1334177-86-4,1-(2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)-3-oxo-7,10,13,16,19,22,25,28-octaoxa-4-azahentriacontan-31-oic acid,as a common compound, the synthetic route is as follows.

Piperidine (0.2 mL) was added to a solution of 90 (77 mg, 63.4 mumomicronIota) in DMF (1 mL). The reaction mixture was allowed to stir for 20 minutes. The reaction mixture was carefully diluted with DCM (50 mL) and washed with water (50 mL). The organic layers was washed with brine (100 mL), dried over MgSO4, filtered and evaporated under reduced pressure to provide the unprotected valine intermediate. The crude residue was immediately redissolved in chloroform (5 mL). Mal(Peg)8-acid (56 mg, 95 mumomicronIota) and EDCI (18 mg, 95 mumomicronIota) were added, followed by methanol (0.1 mL). The reaction was allowed to stir for 3 hours at room temperature at which point completion was observed by TLC and LC/MS (1 .19 min (ES+) m/z (relative intensity) 784.25 (([M + 2H] 2+)/2, 100)). The reaction mixture was diluted with chloroform (50 mL), washed with water (100 mL), dried (MgS04), filtered and evaporated in vacuo, followed by high vacuum drying, to provide the crude product. Purification by flash chromatography (gradient elution: HPLC grade 96:4 v/v CHCl3/MeOH to 90:10 v/v CHCl3/MeOH) gave 91 as a yellow solid (43 mg, 43%). 1H NMR (400 MHz, CDCI3) delta 8.73 (s, 1 H), 7.88 (dd, J = 7.6, 3.9 Hz, 2H), 7.75 (d, J = 8.6 Hz, 2H), 7.52 (d, J = 2.0 Hz, 2H), 7.44 (s, 1 H), 7.40 – 7.28 (m, 4H), 6.91 (d, J = 8.8 Hz, 2H), 6.81 (s, 2H), 6.69 (s, 2H), 6.48 (s, 1 H), 4.72 – 4.63 (m, 1 H), 4.46 – 4.34 (m, 2H), 4.25 – 4.03 (m, 6H), 3.95 (s, 4H), 3.84 (dd, J = 17.2, 10.1 Hz, 4H), 3.72 – 3.46 (m, 30H), 3.44 – 3.32 (m, 4H), 3.30 – 3.20 (m, 4H), 2.75 – 2.63 (m, 1 H), 2.59 (s, 4H), 2.55 – 2.43 (m, 3H), 2.37 (s, 3H), 2.29 (dd, J = 12.7, 6.7 Hz, 1 H), 2.03 – 1 .89 (m, 4H), 1 .72 (d, J = 22.7 Hz, 8H), 1 .46 (d, J = 7.2 Hz, 3H), 1 .01 (dd, J = 1 1 .5, 6.9 Hz, 6H). MS (ES+) m/z (relative intensity) 784.25 (([M + 2H] 2+)/2, 100)., 1334177-86-4

The synthetic route of 1334177-86-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; VAN BERKEL, Patricius Hendrikus Cornelis; HOWARD, Philip Wilson; (283 pag.)WO2016/166298; (2016); A1;,
Pyrroline – Wikipedia
1-Pyrroline | C4H7N – PubChem

1334177-86-4, 1-(2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)-3-oxo-7,10,13,16,19,22,25,28-octaoxa-4-azahentriacontan-31-oic acid is a pyrrolines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,1334177-86-4

(e) N-((S)- 1-(((S)- 1-((4-((S)-8-(3-(((S) -2-(Benzo[d][1, 3]dioxol-5-yI) – 7-methoxy-5-oxo-5, 1 ladihydro- 1H-pyrrolo[2, 1-c][1, 4]benzodiazepin-8-yI) oxy) propoxy)- 7-methoxy-5-oxo-5, 1 ladihydro- 1H-pyrrolo[2, 1-c][1, 4]benzodiazepin-2-yI)phenyl)amino)- 1-oxopropan-2-yI)amino)-3- methyl- 1-oxobutan-2-yl)- 1-(3-(2, 5-dioxo-2, 5-dihydro- 1H-pyrrol- 1-yl)propanamido)- 3,6,9, 12,15, 18,21, 24-octaoxaheptacosan-2 7-amide (33)The imine 32 (92 mg, 0.1 mmol, 1.1 equiv.) was dissolved in CHCI3 (6 mL) with one drop of anhydrous MeOH to aid dissolution. Maleimide-PEG8-acid (53 mg, 0.09 mmol, 1 equiv.) was added followed by EEDQ (33 mg, 0.14 mmol, 1.5 equiv.). This was left to stir vigorously at room temperature under Ar for 4 days until LC/MS analysis showed majority product formation. The solvent was removed in vacuo and the crude product was partially purified by silica gel column chromatography (CHCI3 with 1% to 10% MeOH gradient) yielding 33 (81mg). The material was purified further by preparative HPLC to give 33 as a yellow solid (26.3 mg, 18%). Fast Formic run: LC/MS (1.39 mm (ES+) mlz (relative intensity) 1485.00 ([M + H]+., 64).

1334177-86-4 1-(2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)-3-oxo-7,10,13,16,19,22,25,28-octaoxa-4-azahentriacontan-31-oic acid 51340955, apyrrolines compound, is more and more widely used in various fields.

Reference£º
Patent; CANCER RESEARCH TECHNOLOGY LIMITED; VAN BERKEL, Patricius Henrikus Cornelis; HOWARD, Philip Wilson; WILLIAMS, David G; WO2015/159076; (2015); A1;,
Pyrroline – Wikipedia
1-Pyrroline | C4H7N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1334177-86-4,1-(2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)-3-oxo-7,10,13,16,19,22,25,28-octaoxa-4-azahentriacontan-31-oic acid,as a common compound, the synthetic route is as follows.

N-(3-Dimethylaminopropyl)-N’-ethylcarbodiimide (28 mg, 0.146 mmol, 1 eq) was added to a solution of 42 (203 mg, 0.146 mmol) and maleimide-PEGs acid (87 mg, 0.146 mmol) in chloroform (5 ml_). The reaction was stirred for 1 .5 h then diluted with chloroform (50 ml_), washed with water (50 ml_), brine (30 ml_), dried over magnesium sulphate, filtered and evaporated. Flash chromatography [gradient elution 100% DCM to 90% DCM/10% methanol] gave 43 as a pale yellow solid (205 mg, 72%). LC/MS, System 1 : RT 5.75 min; MS (ES+) m/z (relative intensity) 982.90 (100), 1963.70 (5)., 1334177-86-4

As the paragraph descriping shows that 1334177-86-4 is playing an increasingly important role.

Reference£º
Patent; SPIROGEN SARL; HOWARD, Philip, Wilson; EZEADI, Ebele; D’HOOGE, Francois; PATEL, Neki; KEMP, Gary; WO2015/52322; (2015); A1;,
Pyrroline – Wikipedia
1-Pyrroline | C4H7N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1334177-86-4,1-(2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)-3-oxo-7,10,13,16,19,22,25,28-octaoxa-4-azahentriacontan-31-oic acid,as a common compound, the synthetic route is as follows.

N-(3-Dimethylaminopropyl)-N’-ethylcarbodiimide (28 mg, 0.146 mmol, 1 eq) was added to a solution of 105 (203 mg, 0.146 mmol) and maleimide-PEG8 acid (87 mg, 0.146 mmol) in chloroform (5 mL). The reaction was stirred for 1 .5 h then diluted with chloroform (50 mL), washed with water (50 mL), brine (30 mL), dried over magnesium sulphate, filtered and evaporated. Flash chromatography [gradient elution 100% DCM to 90% DCM/10% methanol] gave 106 as a pale yellow solid (205 mg, 72%). LC/MS: RT 5.75 min; MS (ES+) m/z (relative intensity) 982.90 (100), 1963.70 (5)., 1334177-86-4

The synthetic route of 1334177-86-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; VAN BERKEL, Patricius Hendrikus Cornelis; HOWARD, Philip Wilson; (308 pag.)WO2016/166304; (2016); A1;,
Pyrroline – Wikipedia
1-Pyrroline | C4H7N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1334177-86-4,1-(2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)-3-oxo-7,10,13,16,19,22,25,28-octaoxa-4-azahentriacontan-31-oic acid,as a common compound, the synthetic route is as follows.

EDCI .HCI (0.13 g, 0.66 mmol, 1 .1 eq.) was added to a cloudy solution of compound 21 (0.61 g, 0.6 mmol, 1 .0 eq.) and Mal-dPEG8-OH (0.393 g, 0.66 mmol, 1 .1 eq.) in CHCI3 (25 mL). The clear solution was stirred at room temperature for 1 .5h., diluted with CHC (100 mL) washed with brine (2 x 100 mL), dried (MgS04) and evaporated under reduced pressure to give a yellow foam. Purification by flash column chromatography [CHCb/MeOH 0% to 6% in 1 % increments gave the product as a white foam (0.786 g, 82%). Analytical Data: RT 1 .44 min; MS (ES+) m/z (relative intensity) 1586 {[M + H]+ ,40), 1609 {[M + Na]+ , 100)

1334177-86-4, As the paragraph descriping shows that 1334177-86-4 is playing an increasingly important role.

Reference£º
Patent; MEDIMMUME LIMITED; HOWARD, Philip Wilson; DUNNY, Elizabeth; MASTERSON, Luke; (151 pag.)WO2017/137553; (2017); A1;,
Pyrroline – Wikipedia
1-Pyrroline | C4H7N – PubChem

1334177-86-4, 1-(2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)-3-oxo-7,10,13,16,19,22,25,28-octaoxa-4-azahentriacontan-31-oic acid is a pyrrolines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Piperidine (0.2 mL) was added to a solution of 90 (77 mg, 63.4 pmol) in DMF (1 mL). The reaction mixture was allowed to stir for 20 minutes. The reaction mixture was carefully diluted with DCM (50 mL) and washed with water (50 mL). The organic layers was washed with brine (100 mL), dried over Mg504, filtered and evaporated under reduced pressure to provide the unprotected valine intermediate. The crude residue was immediately redissolved in chloroform (5 mL). Mal(Peg)8-acid (56 mg, 95 pmol) and EDCI (18 mg, 95 pmol) were added, followed by methanol (0.1 mL). The reaction was allowed to stir for 3 hours at room temperature at which point completion was observed by TLC and LC/MS (1.19 mm (ES+) m/z(relative intensity) 784.25 (([M+ 2H]2)/2, 100)). The reaction mixture was diluted with chloroform (50 mL), washed with water (100 mL), dried (MgSO4), filtered and evaporated in vacuo, followed by high vacuum drying, to provide the crude product. Purification by flash chromatography (gradient elution: HPLC grade 96:4 v/v CHCI3/MeOH to 90:10 v/v CHCI3/MeOH) gave 91 as a yellow solid (43 mg, 43%). 1H NMR (400 MHz, ODd3) 6 8.73 (s, 1 H), 7.88 (dd, J = 7.6, 3.9 Hz, 2H), 7.75 (d, J = 8.6 Hz, 2H), 7.52 (d, J = 2.0 Hz, 2H), 7.44 (s, 1 H), 7.40 – 7.28 (m, 4H), 6.91 (d, J = 8.8 Hz, 2H), 6.81 (s, 2H), 6.69 (s, 2H),6.48 (s, 1 H), 4.72 – 4.63 (m, 1 H), 4.46 – 4.34 (m, 2H), 4.25 – 4.03 (m, 6H), 3.95 (s, 4H), 3.84 (dd, J 17.2, 10.1 Hz, 4H), 3.72-3.46 (m, 30H), 3.44-3.32 (m, 4H), 3.30-3.20 (m, 4H), 2.75 – 2.63 (m, 1 H), 2.59 (s, 4H), 2.55 – 2.43 (m, 3H), 2.37 (s, 3H), 2.29 (dd, J = 12.7, 6.7 Hz, 1 H), 2.03 – 1.89 (m, 4H), 1.72 (d, J = 22.7 Hz, 8H), 1.46 (d, J = 7.2 Hz, 3H), 1.01 (dd, J = 11 .5, 6.9 Hz, 6H). MS (ES) m/z (relative intensity) 784.25 (([M + 2H] 2+)/2, 100).

1334177-86-4, The synthetic route of 1334177-86-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; VAN BERKEL, Patricius Hendrikus Cornelis; HOWARD, Philip Wilson; (290 pag.)WO2016/166299; (2016); A1;,
Pyrroline – Wikipedia
1-Pyrroline | C4H7N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1334177-86-4,1-(2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)-3-oxo-7,10,13,16,19,22,25,28-octaoxa-4-azahentriacontan-31-oic acid,as a common compound, the synthetic route is as follows.

A solution of compound 39 (0.136 g, 0.1 mmol, 1 .0 eq.), Mal-dPEG8-OH (0.066 g, 0.1 1 mmol, 1.1 eq.) and EDCI.HCI (0.022 g, 0.1 1 mmol, 1.1 eq.) in dry DCM (10 mL) and MeOH (1 drop) was stirred at room temperature for 1.45h. The reaction mixture was diluted with CHC and washed with water, brine, dried (MgS04) and evaporated under reduced pressure to give the crude product. Purification by flash column chromatography [CHC /MeOH 1 % to 9%] gave the product as a white solid (0.123 g, 63%). Analytical Data: [a]21D = +1 12.5 (c = 0.4, hplc CHCI3); RT 6.37 min; MS (ES+) m/z (relative intensity) 1936 {[M + 1]+ , 35); 1958 {[M + Na]+ , 15)., 1334177-86-4

The synthetic route of 1334177-86-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MEDIMMUME LIMITED; HOWARD, Philip Wilson; DUNNY, Elizabeth; MASTERSON, Luke; (151 pag.)WO2017/137553; (2017); A1;,
Pyrroline – Wikipedia
1-Pyrroline | C4H7N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1334177-86-4,1-(2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)-3-oxo-7,10,13,16,19,22,25,28-octaoxa-4-azahentriacontan-31-oic acid,as a common compound, the synthetic route is as follows.

Piperidine (0.2 mL) was added to a solution of 25 (77 mg, 63.4 pmol) in DMF (1 mL). The reaction mixture was allowed to stir for 20 minutes. The reaction mixture was carefullydiluted with DCM (50 mL) and washed with water (50 mL). The organic layers was washed with brine (100 mL), dried over Mg504, filtered and evaporated under reduced pressure to provide the unprotected valine intermediate. The crude residue was immediately redissolved in chloroform (5 mL). Mal(Peg)8-acid (56 mg, 95 pmol) and EDCI (18 mg, 95 pmol) were added, followed by methanol (0.1 mL). The reaction was allowed to stir for 3 hours at room temperature at which point completion was observed by TLC and LC/MS(1.19 mm (ES+) m/z (relative intensity) 784.25 (([M + 2H]2)/2, 100)). The reaction mixture was diluted with chloroform (50 mL), washed with water (100 mL), dried (MgSO4), filtered and evaporated in vacuo, followed by high vacuum drying, to provide the crude product. Purification by flash chromatography (gradient elution: HPLC grade 96:4 v/v CHCI3/MeOH to 90:10 v/v CHCI3/MeOH) gave 26 as a yellow solid (43 mg, 43%). 1H NMR (400 MHz, CDCI3)58.73 (s, IH), 7.88 (dd, J= 7.6, 3.9 Hz, 2H), 7.75 (d, J= 8.6 Hz, 2H), 7.52 (d, J= 2.0 Hz,2H), 7.44 (s, I H), 7.40 – 7.28 (m, 4H), 6.91 (d, J = 8.8 Hz, 2H), 6.81 (s, 2H), 6.69 (s, 2H),6.48 (s, I H), 4.72 – 4.63 (m, I H), 4.46 – 4.34 (m, 2H), 4.25 – 4.03 (m, 6H), 3.95 (s, 4H), 3.84(dd, J= 17.2, 10.1 Hz, 4H), 3.72-3.46 (m, 30H), 3.44-3.32 (m, 4H), 3.30-3.20 (m, 4H),2.75 – 2.63 (m, I H), 2.59 (s, 4H), 2.55 – 2.43 (m, 3H), 2.37 (s, 3H), 2.29 (dd, J = 12.7, 6.7Hz, IH), 2.03-1.89 (m, 4H), 1.72 (d, J= 22.7 Hz, 8H), 1.46 (d, J= 7.2 Hz, 3H), 1.01 (dd, J = 11 .5, 6.9 Hz, 6H). MS (ES) m/z (relative intensity) 784.25 (([M + 2H] 2+)/2 100)., 1334177-86-4

The synthetic route of 1334177-86-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; SPIROGEN SARL; ADC THERAPEUTICS SARL; HOWARD, Philip Wilson; VAN BERKEL, Patricius Hendrikus Cornelis; WO2015/52533; (2015); A1;; ; Patent; SPIROGEN SARL; ADC THERAPEUTICS SARL; HOWARD, Philip Wilson; VAN BERKEL, Patricius Hendrikus Cornelis; WO2015/52534; (2015); A1;,
Pyrroline – Wikipedia
1-Pyrroline | C4H7N – PubChem

1334177-86-4, 1-(2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)-3-oxo-7,10,13,16,19,22,25,28-octaoxa-4-azahentriacontan-31-oic acid is a pyrrolines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EDCI.HCI (117 mg, 0.29 mmol) was added to a stirred solution of MAL-dPEG8-acid (360mg, 0.6079 mmol, Stratech Scientific Limited) and amine 120 (608 mg, 0.5526 mmol) inCH2CI2 (15 mL) at room temperature. The reaction mixture was stirred under an argon atmosphere for 24 hours, at which point analysis by LC/MS showed complete consumption of 120. The reaction mixture was diluted with CH2CI2 and washed successively with sat. NH4CI and sat. NaH 003, dried over Mg504, and concentrated in vacuo to provide thecrude product. Purification by lsoleraTM (4-16% MeOH in CH2CI2) gave amide 121 as a white solid (77 mg, 79% purity (UV integration 223 nm) 8.8% crude yield; 107 mg, 88% purity, 12% crude yield; 224 mg, 86% purity, 25% crude yield)., 1334177-86-4

As the paragraph descriping shows that 1334177-86-4 is playing an increasingly important role.

Reference£º
Patent; MEDIMMUNE LIMITED; HOWARD, Philip Wilson; GREGSON, Stephen John; (207 pag.)WO2018/192944; (2018); A1;,
Pyrroline – Wikipedia
1-Pyrroline | C4H7N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1334177-86-4,1-(2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)-3-oxo-7,10,13,16,19,22,25,28-octaoxa-4-azahentriacontan-31-oic acid,as a common compound, the synthetic route is as follows.

EDCI hydrochloride (8 mg, 0.042 mmol) was added to a suspension of Maleimide-PEG8-acid(25 mg, 0.042 mmol) in dry CH2CI2 (4 mL) under argon atmosphere. PBD 19 (42 mg, crude)was added straight away and stirring was maintained until the reaction was complete (3hours). The reaction was diluted with CH2CI2 and the organic phase was washed with H20 and brine before being dried over MgSO4, filtered and excess solvent removed by rotary evaporation under reduced pressure by rotary evaporation under reduced pressure. The product was purified by careful silica gel chromatography (slow elution starting with 100%CHCI3 up to 9:1 CHCI3/MeOH) followed by reverse phase HPLC to remove unreacted maleimide-PEG8-acid. The product 20 was isolated in 10% over two steps (6.6 mg). LC/MS 1.16 mm (ES+) m/z (relative intensity) 770.20 ([M + 2H], 40%)., 1334177-86-4

As the paragraph descriping shows that 1334177-86-4 is playing an increasingly important role.

Reference£º
Patent; SPIROGEN SARL; ADC THERAPEUTICS SARL; HOWARD, Philip Wilson; VAN BERKEL, Patricius Hendrikus Cornelis; WO2015/52532; (2015); A1;,
Pyrroline – Wikipedia
1-Pyrroline | C4H7N – PubChem