The present invention relates to process for preparation of ledipasvir of formula 1 and its novel intermediates. The process involves reaction of compound of formula 2 with compound of formula 3 to yield a compound of formula 4, deprotection of compound of formula 4 to yield compound of formula 5 and conversion of compound of formula 5 to Ledipasvir wherein PG is an amine protecting group provided that amino protecting group is not carbomethyloxy (-COOCH3) group; X and Y are leaving groups.
本发明涉及制备式1的来替帕韦及其新型中间体的过程。该过程涉及将式2的化合物与式3的化合物反应,得到式4的化合物,去保护式4的化合物得到式5的化合物,再将式5的化合物转化为来替帕韦,其中
PG是
氨基保护基,但不是羧甲氧基(-COOCH3)基;X和Y是离去基。