摘要 |
<p>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.</p> |
申请人 |
MATRIX LABORATORIES LTD.;RAMA, SHANKAR;GORANTLA, SARAT, CHANDRA, SRIKANTH;VADALI, LAKSHMANA, RAO;INUPAKUTIKA, VENKATA, BALA, KISHORE, SARMA;DASARI, SRINIVAS, RAO;MITTAPELLY, NAGARAJU;SINGH, SANTOSH, KUMAR;DATTA, DEBASHISH |
发明人 |
RAMA, SHANKAR;GORANTLA, SARAT, CHANDRA, SRIKANTH;VADALI, LAKSHMANA, RAO;INUPAKUTIKA, VENKATA, BALA, KISHORE, SARMA;DASARI, SRINIVAS, RAO;MITTAPELLY, NAGARAJU;SINGH, SANTOSH, KUMAR;DATTA, DEBASHISH |