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NOVEL PROCESS FOR THE PREPARATION OF CIS-NUCLEOSIDE DERIVATIVE
专利权人:
Shankar Rama
发明人:
Shankar Rama,Sarat Chandra Srikanth Gorantla,Lakshmana Rao Vadali,Venkata Bala Kishore Sarma Inupakutika,Srinivas Rao Dasari,Nagaraju Mittapelly,Santosh Kumar Singh,Debashish Datta
申请号:
US13577118
公开号:
US20120295930A1
申请日:
2011.02.01
申请国别(地区):
US
年份:
2012
代理人:
摘要:
The present invention relates to an improved process for the preparation of cis-nucleoside derivative of formula-1 involving chlorination of the compound of formula-2 followed by reaction with compound of formula-3 in presence of a base to get compound of formula-4, reacting the compound of formula-4 with an alkyl halide (RiX) to get a quaternary ammonium salt then with cytosine derivative of formula-5 to provide the compound of formula-6, optionally de-protecting the compound of formula-6 to the compound of formula-7, reducing compound of formula-7 with metal catalyst in presence of a buffer solution, then adding an organic acid to get the compound of formula-8, and converting the compound of formula-8 to cis-nucleoside derivative of formula-1. The present invention further relates to novel cis-nucleoside derivative of formula-8. The present invention also relates to a pharmaceutical composition comprising cis-nucleoside derivative of formula-1 with excipients.
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