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The present invention relates to bifunct...
L-4-hydroxyproline methyl ester hydrochloride
(2S,4R)-1-[(2S)-2-{2-[3-(2-{2-[(9S)-7-(4-chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetraazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-9-yl]acetamido}ethoxy)propoxy]acetamido}-3,3-dimethylbutanoyl]-4-hydroxy-N-[(1S)-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]ethyl]pyrrolidine-2-carboxamide
| Conditions | Yield |
|---|---|
|
Multi-step reaction with 5 steps
1.1: N-ethyl-N,N-diisopropylamine; HATU / N,N-dimethyl-formamide / 18 h / 0 - 20 °C / Inert atmosphere
2.1: lithium hydroxide monohydrate; water / tetrahydrofuran / 18 h / 20 °C
2.2: pH 2-3
3.1: N-ethyl-N,N-diisopropylamine; HATU / tetrahydrofuran / 2 h / 0 - 20 °C
4.1: hydrogenchloride / methanol / 3 h / 20 °C
5.1: N-ethyl-N,N-diisopropylamine; HATU / N,N-dimethyl-formamide / 0.33 h / 0 - 20 °C
With
hydrogenchloride; lithium hydroxide monohydrate; water; N-ethyl-N,N-diisopropylamine; HATU;
In
tetrahydrofuran; methanol; N,N-dimethyl-formamide;
|
(2S,4R)-1-((S)-2-amino-3,3-dimethylbutanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide hydrochloride
(S)-2-(3-(2-(2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetamido)ethoxy)propoxy)acetic acid
(2S,4R)-1-[(2S)-2-{2-[3-(2-{2-[(9S)-7-(4-chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetraazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-9-yl]acetamido}ethoxy)propoxy]acetamido}-3,3-dimethylbutanoyl]-4-hydroxy-N-[(1S)-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]ethyl]pyrrolidine-2-carboxamide
| Conditions | Yield |
|---|---|
|
With
N-ethyl-N,N-diisopropylamine; HATU;
In
N,N-dimethyl-formamide;
at 0 - 20 ℃;
for 0.333333h;
|
404.1 mg |
N-tert-butyloxycarbonyl-L-tert-leucine
(2S,4R)-1-[(2S)-2-[(tert-butoxycarbonyl)amino]-3,3-dimethylbutanoyl]-4-hydroxypyrrolidine-2-carboxylic acid
methyl (2S.4R)-1-[(2S)-2-{[(tert-butoxy)carbonyl]amino}-3.3-dimethylbutanoyl]-4-hydroxypyrrolidine-2-carboxylate
3-[2-(benzyloxy)ethoxy]-1-propanol