1147103-42-1Relevant articles and documents
Telaprevir intermediate preparation method
-
, (2017/08/31)
The invention discloses a telaprevir intermediate preparation method. A telaprevir intermediate is a formula I compound, and a reaction route is as shown in the specification, wherein R is selected from C1-C4 alkyl groups, R1 is selected from hydrogen, C1-C8 alkyl groups, C1-C8 alkoxy groups, C6-C12 aryl groups, alkyl sulfonyl, C6-C12 aryl sulfonyl groups or substituted C6-C12 aryl sulfonyl groups, and P is an amino protection group. The method has advantages of simplicity in operation, safety, freeness of pollution and special requirements on equipment, low production cost, high yield and the like, is suitable for large-scale production and has a high practical value in realization of telaprevir industrialization.
A process for the preparation of intermediates telaprevir
-
, (2017/03/14)
The invention provides a telaprevir intermediate preparation method. The telaprevir intermediate preparation method comprises the following steps: (1) synthesizing (3aR, 6aS)-1,3a,4,5,6,6a-hexahydrocyclopentapyrrol; (2) synthesizing (3aR, 6aS)-octahydrocyclopentapyrrol-1-sodium sulfate; (3) synthesizing (3aR, 6aS)- octahydrocyclopentapyrrol-1-cyanogen; (4) synthesizing (3aR, 6aS)- octahydrocyclopentapyrrol-1-carboxylic acid; (5) synthesizing (3aR, 6aS)-2-Boc octahydrocyclopentapyrrol-1-carboxylic acid; (6) synthesizing (1s, 3aR, 6aS)-2-Boc octahydrocyclopentapyrrol-1-carboxylic acid; (7) synthesizing (1s, 3aR, 6aS)-2-Boc octahydrocyclopentapyrrol-1-carboxylic acid ethyl ester salt. The telaprevir intermediate preparation method is reasonable in process, low in cost and simple and convenient to operate, reagents are inexpensive and easy to obtain, and the control on reaction is easy.