title: A highly convergent and efficient synthesis of a macrocyclic hepatitis C virus protease inhibitor BI 201302.
abstract: A highly convergent large scale synthesis of a 15-membered macrocyclic hepatitis C virus (HCV) protease inhibitor BI 201302 was achieved, in which the key features are the practical macrocyclization by Ru-catalyzed ring-closing metathesis (0.1 mol % Grela catalyst, 0.1-0.2 M concentration) and the efficient sulfone-mediated SNAr reaction.
authors: Chemical Development, Boehringer-Ingelheim Pharmaceuticals, 900 Ridgebury Road, Ridgefield, Connecticut 06877, USA. xudong.wei@boehringer-ingeheim.com
authors: Xudong
authors: X
authors: Wei
authors: Chutian
authors: C
authors: Shu
authors: Nizar
authors: N
authors: Haddad
authors: Xingzhong
authors: X
authors: Zeng
authors: Nitinchandra D
authors: ND
authors: Patel
authors: Zhulin
authors: Z
authors: Tan
authors: Jianxiu
authors: J
authors: Liu
authors: Heewon
authors: H
authors: Lee
authors: Sherry
authors: S
authors: Shen
authors: Scot
authors: S
authors: Campbell
authors: Richard J
authors: RJ
authors: Varsolona
authors: Carl A
authors: CA
authors: Busacca
authors: Azad
authors: A
authors: Hossain
authors: Nathan K
authors: NK
authors: Yee
authors: Chris H
authors: CH
authors: Senanayake
mesh_terms: D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002384:Catalysis; D003500:Cyclization; D016174:Hepacivirus / Q000187:drug effects*; D015394:Molecular Structure; D010456:Peptides, Cyclic / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011480:Protease Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000998:Antiviral Agents; C581612:BI 201302; D010456:Peptides, Cyclic; D011480:Protease Inhibitors