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Process and intermediates for the preparation of a

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专利名称:Process and intermediates for the

preparation of an antiviral agent containing acyclobutyl group

发明人:Godfrey, Jollie D., Jr.,Mueller, Richard

H.,Kissick, Thomas P.,Singh, Janak

申请号:EP92115827.5申请日:19920916公开号:EP05348A2公开日:19930407

摘要:Racemic Feist's acid is treated with (R)-(+)-a-methylbenzylamine to yield (1R-trans)-3-methylenecyclopropane-1,2-dicarboxylic acid, (R)-a-methylbenzylamine (1:1) salt.This salt can then be converted to (1R-trans)-3-methylene-1,2-cyclopropanedicarboxylicacid, dimethyl ester which is an intermediate in the preparation of the antiviral agent Ä1R-(1a,2b,3a)Ü-2-amino-9-Ä2,3-bis(hydroxymethyl)cyclobutylÜ-1,9-dihydro-6H-purin-6-one.The improved process also enables the recovery of racemic Feist's acid from theresolution.

申请人:E.R. SQUIBB & SONS, INC.

地址:P.O.Box 4000 Princeton New Jersey 083-4000 US

国籍:US

代理机构:Josif, Albert, Dr.-Ing.

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