Process Research and Development of an Enantiomerically Enriched Allyic Amine, One of the Key Intermediates for the Manufacture of Synthetic Tetracyclines
A robust, cost-effective, and high yielding manufacturing process for enantiomerically enriched (S)-allylic amine 3, a key intermediate for fully synthetic tetracyclines have been developed. Two novel and scalable asymmetric vinylations resulting in high-to-excellent stereoselectivity have been developed for the key step. The final product is purified by an efficient crystallization of a l-tartaric salt. The process described has been used to manufacture ~350 kg of the tartaric salt of 3 with 99.0% ee in 8 steps (35% overall yield) from cheap and readily available dimethyl maleate.
Zhang, Wu-Yan,Hogan, Philip C.,Chen, Chi-Li,Niu, John,Wang, Zhimin,Lafrance, Danny,Gilicky, Olga,Dunwoody, Nicholas,Ronn, Magnus
p. 1784 - 1795
(2015/12/01)
DERIVATIVES OF N-ACYL-N'-PHENYLPIPERAZINE USEFUL (INTER ALIA) FOR THE PROPHYLAXIS OR TREATMENT OF DIABETES
The present invention relates to a compound represented by the formula wherein each symbol is as defined in the present specification, which has a superior RBP4-lowering action and is useful as a pharmaceutical composition for the prophylaxis or treatment of a disease or condition mediated by an increase in RBP4.
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(2012/04/04)
ISOXAZOLE DERIVATIVE AND ISOTHIAZOLE DERIVATIVE HAVING INHIBITORY ACTIVITY ON 11 BETA -HYDROXYSTEROID DEHYDROGENASE TYPE I
Disclosed is a compound useful as an inhibitor of 11β-hydroxysteroid dehydrogenase type 1. A compound represented by the formula: a pharmaceutically acceptable salt or solvate thereof, wherein R1 is a group of the formula: -C(=O)NR4R
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(2009/01/24)
HETEROCYCLIC COMPOUND HAVING TYPE I 11 BETA HYDROXYSTEROID DEHYDROGENASE INHIBITORY ACTIVITY
Disclosed is a compound useful as a type I 11 β hydroxysteroid dehydrogenase inhibitor. A compound represented by the formula: a pharmaceutically acceptable salt or solvate thereof, wherein R1 is optionally substituted cycloalkyl, optionally su
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(2010/11/30)
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