公开(公告)号：US5264574A

公开(公告)日：1993-11-23

申请号：US862647

申请日：1992-04-03

Applicant: James D. Carroll ,  David J. Mathre ,  Edward G. Corley ,  Andrew S. Thompson

Inventor： James D. Carroll ,  David J. Mathre ,  Edward G. Corley ,  Andrew S. Thompson

IPC: C07F5/02 ,  C07D235/02

CPC classification number: C07F5/025

Abstract: Oxazaborolidine-borane complexes are prepared by adding a C.sub.5-8 alkane, typically hexane, to an aged solution of oxazaborolidine and a source of borane such as borane-dimethyl sulfide or gaseous diborane to crystallize the oxazaborolidine complex.

Abstract translation: 通过将C5-8烷烃（通常为己烷）加入恶唑硼烷和硼烷如硼烷 - 二甲基硫醚或气态乙硼烷的老化溶液中以使所述恶唑硼烷复合物结晶来制备恶唑硼烷 - 硼烷配合物。

公开(公告)号：US5157129A

公开(公告)日：1992-10-20

申请号：US510804

申请日：1990-04-18

Applicant: Thomas J. Blacklock ,  Todd K. Jones ,  Edward J. J. Grabowski ,  David J. Mathre ,  Julie J. Mohan ,  Paul Sohar ,  F. Edward Roberts ,  Lyndon C. Xavier

Inventor： Thomas J. Blacklock ,  Todd K. Jones ,  Edward J. J. Grabowski ,  David J. Mathre ,  Julie J. Mohan ,  Paul Sohar ,  F. Edward Roberts ,  Lyndon C. Xavier

IPC: A61K31/38 ,  A61P27/02 ,  B01J31/02 ,  C07B53/00 ,  C07B61/00 ,  C07D207/08 ,  C07D495/04 ,  C07F5/02

CPC classification number: C07D207/08 ,  C07D495/04

Abstract: 5,6-Dihydro-4-(R-amino)-4H-thieno[2,3-b]-thiopyran-2-sulfonamide-7,7-dioxide is a potent carbonic anhydrase inhibitor useful in the treatment of ocular hypertension and glaucoma. The S-(+)-enantiomer of that compound, the more active enantiomer, is prepared by a process involving an intermediate step of an enantioselective reduction of a carbonyl group employing an oxazaborolidine chiral catalyst.

公开(公告)号：US5039802A

公开(公告)日：1991-08-13

申请号：US510768

申请日：1990-04-18

Applicant: Thomas J. Blacklock ,  Todd K. Jones ,  David J. Mathre ,  Lyndon C. Xavier

Inventor： Thomas J. Blacklock ,  Todd K. Jones ,  David J. Mathre ,  Lyndon C. Xavier

IPC: B01J31/02 ,  C07D207/06 ,  C07D207/08 ,  C07D211/04 ,  C07D215/04 ,  C07D495/04 ,  C07D498/04 ,  C07F5/02

CPC classification number: C07D207/08 ,  C07D495/04 ,  C07F5/02 ,  C07F5/025

Abstract: The chiral catalyst of general structure 1, or its enantiomer ##STR1## is prepared by treating the corresponding N-carboxy anhydride of structure 2 ##STR2## with an aryl metal, especially a phenyl metal such as an aryl magnesium halide, aryl lithium, aryl zinc or aryl cesium, to form a 1,1-diaryl-methanol of structure 3 ##STR3## followed by treatment with a compound of structure, 4 ##STR4## The catalyst, wherein R is aromatic, is novel and in some cases superior to the catalyst wherein R is alkyl or aralkyl in directing the chirality of borane-dimethyl sulfide reductions of ketones to secondary alcohols.