27-04-2017 дата публикации
Номер: US20170114087A1
Автор:
Yanling Wang,
Yuan Wang,
Xungui He,
Chuanjun Liu,
Jirang Zhu,
Jie Li,
Qingzhong Cheng,
Mingyong Yuan,
WANG YANLING,
WANG YUAN,
HE XUNGUI,
LIU CHUANJUN,
ZHU JIRANG,
LI JIE,
CHENG QINGZHONG,
YUAN MINGYONG,
Wang Yanling,
Wang Yuan,
He Xungui,
Liu Chuanjun,
Zhu Jirang,
Li Jie,
Cheng Qingzhong,
Yuan Mingyong
Принадлежит:
The invention is directed to processes for synthesizing bicyclic nucleoside antiviral compounds and for synthesizing the intermediates used in the process. The invention is also directed to novel intermediate compounds useful in the process. The antiviral compounds are useful in the treatment of herpes zoster (i.e., varicella zoster virus, VZV, shingles) and for the prevention of post herpetic neuralgia (PHN) resulting from this viral infection. 1. A compound selected from a compound of Formula (V), Formula (VI), Formula (VII), and Formula (VIII): [{'sup': '1', 'sub': 1', '6, 'Ris C-Calkyl;'}, {'sup': 4', '5, 'sub': 1', '2, 'Rand Rare each independently H or C-Calkyl;'}, {'sup': '6', 'Ris an amino acid protecting group selected from the group consisting of Boc, Fmoc, and Cbz;'}, {'sup': '10', 'Ris trityl, 4,4′-dimethoxytrityl, diphenylmethylsilyl, tert-butyldimethylsilyl, or tert-butyldiphenylsilyl; and'}, {'sup': '11', 'claim-text': [{'sub': 1', '6, 'C-Calkanoyl,'}, 'halogen substituted alkanoyl,', 'optionally substituted aroyl,', 'optionally substituted benzyl,', 'Cbz, and', 'diphenylmethyl., 'Ris selected from'}], 'wherein The present application is a continuation of U.S. patent application Ser. No. 14/990,955, filed Jan. 8, 2016 (now allowed), which is a division of U.S. patent application Ser. No. 13/878,303, filed Aug. 20, 2013 (now U.S. Pat. No. 9,260,469), which is a 35 U.S.C. §371 National Phase application of PCT/US2011/055229, filed Oct. 7, 2011, which claims priority to Chinese Patent Application No. 201010506554.0, filed Oct. 9, 2010, and Chinese Patent Application No. 201010556506.2, filed Nov. 16, 2010, the entire disclosures of which are incorporated herein by reference.This application relates to methods for the preparation of a synthetic active pharmaceutical ingredient, FV-100, (S)-((2R,3S,5R)-(3-hydroxy-5-(2-oxo-6-(4-pentylphenyl)furo [2,3-d]pyrimidin-3(2H)-yl)-tetrahedrofuran-2-yl)methyl 2-amino-3-methylbutanoate hydrochloride, a bicyclic ...
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