Patent ID: 6080854
Filing Date: 2000-06-27
Classification: C07D,Y02P

Abstract:
A process of synthesizing a compound of formula 1: ##STR15## wherein P and P' independently represent H or a protecting group, R.sub.1 represents H or C.sub.1-4 alkyl, and Hal represents a halogen selected from the group consisting of F, Cl, Br and I, comprising:reacting a compound of formula 2: ##STR16## wherein P, P', and R.sub.1 are defined above, with an alcohol of the formula, R.sub.2 OH, wherein R.sub.2 is C.sub.1-4 alkyl, C.sub.6-10 aryl or C.sub.5-10 heteroaryl in the presence of an acid catalyst or carbodimide reagent to produce a compound of formula 3: ##STR17## wherein P, P', and R.sub.1 are defined above; and reacting a compound of formula 3 in the presence of a base and a haloalkylating agent selected from the group consisting of ICH.sub.2 Cl, BrCH.sub.2 Cl, TMSCH.sub.2 Cl, and TMSCH.sub.2 Br, wherein TMS is trimethylsilyl, to produce a compound of formula 1.