反应 #1178465

ord-997018bea1be44809299abf2a4035667

反应方程式

CC(C)(C)c1cc(NC(=O)Nc2ccc(-c3cn4c(n3)sc3cc(OC(=O)[C@@H]5CCCN5)ccc34)cc2)no1
(2S)-pyrrolidine-2-carboxylic acid 2-{4-[3-(5-tert-butyl-isoxazol-3-yl)-ureido]-phenyl}-benzo[d]imidazo[2,1-b]thiazol-7-yl ester
CC(C)(C)OC(=O)N1CCC[C@H]1C(=O)O.O=C1CCC(=O)N1O
Boc-L-proline N-hydroxysuccinimide
→
CC(C)[C@@H](N)C(=O)Oc1ccc2c(c1)sc1nc(-c3ccc(NC(=O)Nc4cc(C(C)(C)C)on4)cc3)cn12
(2R)-2-AMINO-3-METHYL-BUTYRIC ACID 2-{4-[3-(5-TERT-BUTYL-ISOXAZOL-3-YL)-UREIDO]-PHENYL}-BENZO[D]IMIDAZO[2,1-B]THIAZOL-7-YL ESTER

反应物

CC(C)(C)c1cc(NC(=O)Nc2ccc(-c3cn4c(n3)sc3cc(OC(=O)[C@@H]5CCCN5)ccc34)cc2)no1
(2S)-pyrrolidine-2-carboxylic acid 2-{4-[3-(5-tert-butyl-isoxazol-3-yl)-ureido]-phenyl}-benzo[d]imidazo[2,1-b]thiazol-7-yl ester
CC(C)(C)OC(=O)N1CCC[C@H]1C(=O)O.O=C1CCC(=O)N1O
Boc-L-proline N-hydroxysuccinimide
—
Compound B6

试剂

无

反应条件

详细条件
See reaction.notes.procedure_details.

实验过程

In a manner similar to Step A, (2S)-pyrrolidine-2-carboxylic acid 2-{4-[3-(5-tert-butyl-isoxazol-3-yl)-ureido]-phenyl}-benzo[d]imidazo[2,1-b]thiazol-7-yl ester was made using Boc-L-proline N-hydroxysuccinimide; LC-MS: ESI 545 (M+H)+. [Compound B6]

来源

DOI: 10.6084/m9.figshare.5104873.v1专利: US08129374B2uspto-grants-2012_03