The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Feb. 16, 1999

Filed:

Jul. 30, 1997
Applicant:
Inventors:

John M Williams, Belle Mead, NJ (US);

Ronald B Jobson, East Brunswick, NJ (US);

Assignee:

Merck & Co., Inc., Rahway, NJ (US);

Attorneys:
Primary Examiner:
Int. Cl.
CPC ...
C07D / ; C07D / ;
U.S. Cl.
CPC ...
540350 ; 548556 ;
Abstract

A process for synthesizing a compound of the formula I: ##STR1## or a pharmaceutically acceptable salt or ester thereof, wherein each P independently represents H or a protecting group, and R.sup.1 and R.sup.2 independently represent H, C.sub.1-10 alkyl, aryl or heteroaryl, or substituted C.sub.1-10 alkyl, aryl or heteroaryl, comprising: reacting the compounds: ##STR2## or a pharmaceutically acceptable salt or ester thereof, and ##STR3## or a pharmaceutically acceptable salt or ester thereof, wherein X represents OP(O)(OR).sub.2, or OSO.sub.2 R, wherein R represents C.sub.1-6 alkyl, aryl or perfluoro C.sub.1-6 alkyl, in the presence of an amine selected from the group consisting of: diisopropylamine (DIPA), dicyclohexylamine (DCHA), 2,2,6,6-tetramethylpiperidine (TMP), 1,1,3,3-tetramethylguanidine (TMG), 1,8-diazabicyclo�4.3.0!undec-7-ene (DBU) and 1,5-diazabicyclo�4.3.0!non-5-ene to produce a compound of formula I.


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