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Comparative molecular field analysis (CoMFA). 1. Effect of shape on binding of steroids to carrier proteins.
The main features of the CoMFA approach, exemplified by analyses of the affinities of 21 varied steroids to corticosteroid and testosterone-binding globulins, and a number of advances in the methodology of molecular graphics are described.
Recent advances in comparative molecular field analysis (CoMFA).
Comparative Molecular Field Analysis (CoMFA) has shown predictive performance and versatility that appear to be unprecedented among computer-based techniques for aiding molecular design.
AAA in KAT/DYKAT processes: first- and second-generation asymmetric syntheses of (+)- and (-)-cyclophellitol.
The utility of effecting KAT/DYKAT processes through the Pd-catalyzed AAA reaction is demonstrated by efficient syntheses of both enantiomers of the potent glycosidase inhibitor cyclophellitol.
Development of a Practical Large-Scale Synthesis of Denagliptin Tosylate
A large-scale synthesis of denagliptin tosylate has been developed. The efficiency of the synthesis has been improved from the initially scaled route by changing the order of steps (performing a
Synthesis of 4-Fluoro-β-(4-fluorophenyl)-l-phenylalanine by an Asymmetric Phase-Transfer Catalyzed Alkylation: Synthesis on Scale and Catalyst Stability
4-Fluoro-β-(4-fluorophenyl)-l-phenylalanine 1 was synthesized by the asymmetric phase-transfer catalyzed alkylation of tert-butyl glycinate-benzophenone Schiff base using the cinchona alkaloid
Efficient Asymmetric Synthesis of N-[(1R)-6-Chloro-2,3,4,9-tetrahydro-1H-carbazol-1-yl]-2-pyridinecarboxamide for Treatment of Human Papillomavirus Infections
An efficient asymmetric synthesis of N-[(1R)-6-chloro-2,3,4,9-tetrahydro-1H-carbazol-1-yl]-2-pyridinecarboxamide 1, a potential treatment for human papillomavirus infections, is described. The key
cis‐5‐Amino‐6‐hydroxycyclohexadiene as a Chiral Building Block: An Asymmetric Synthesis of (−)‐Swainsonine
The four contiguous stereocenters of (−)-swainsonine were efficiently set in a 15-step synthesis with a 15 % overall yield and >99% ee. In order to differeniate the double bond in the key building
A convenient route to heteronaphthacenes
Heteronaphthacenes 1 were prepared in two steps from 1,3-dihydrobenzo[c]thiophene 2,2-dioxide (4) and dienophiles 2 via convenient high-temperature Diels-Alder reactions.