Process for the manufacture of chiral catalysts and their salts

摘要

The present invention provides efficient and economical methods for synthesis of (−)-2-exo-morpholinoisoborne-10-thiol, its enantiomer, and related chiral catalysts. Novel compounds and methods of asymmetric synthesis are also disclosed.

主权项

1. A process for preparing a compound of formula (I)the process comprising:
i) contacting a sulfonamide of formula (II) with a first reducing agent under conditions sufficient to provide a disulfide compound of formula (III)and
ii) contacting the disulfide compound of formula (III) with a second reducing agent under conditions suitable to form a compound of formula (I); wherein R1 and R2 are independently H, benzyl, substituted benzyl, C1-12 alkyl, C3-10 cycloalkyl, C4-9 heterocycloalkyl, C6-10 aryl, or C5-9 heteroaryl; R3 and R4 are independently H, benzyl, substituted benzyl, C1-12 alkyl, C3-10 cycloalkyl, C4-9 heterocycloalkyl, C6-10 aryl, or C5-9 heteroaryl; or optionally R3, R4, and N can together form a C3-10 heterocycle.