Development of a Kilogram-Scale Synthesis of a Novel Anti-HCV Agent, CH4930808

被引：5

作者：

Haneishi, Tsuyoshi ^{[1
]}

Kato, Yoshiaki ^{[2
]}

Fukuda, Hiroshi ^{[1
]}

Shimamura, Tomoyuki ^{[2
]}

Tanokura, Takemi ^{[2
]}

Hiraide, Akira ^{[2
]}

Koyama, Kaichiro ^{[2
]}

Fudesaka, Masato ^{[2
]}

Maeda, Kenji ^{[2
]}

Nakata, Nobuyuki ^{[2
]}

Nagase, Masahiro ^{[2
]}

Yabuzaki, Takahiko ^{[2
]}

Takao, Hiroaki ^{[2
]}

Kigawa, Masaharu ^{[2
]}

Shimizu, Hitoshi ^{[2
]}

Shimizu, Makoto ^{[3
]}

机构：

[1] Chugai Pharmaceut Co Ltd, Res Div, 1-135 Komakado, Gotemba, Shizuoka 4128513, Japan

[2] Chugai Pharmaceut Co Ltd, Pharmaceut Technol Div, Kita Ku, 5-5-1 Ukima, Tokyo 1158543, Japan

[3] Mie Univ, Grad Sch Engn, Dept Chem Mat, Tsu, Mie 5148507, Japan

来源：

ORGANIC PROCESS RESEARCH & DEVELOPMENT | 2018年 / 22卷 / 02期

关键词：

D O I：

10.1021/acs.oprd.7b00383

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

Herein, we report the kilogram-scale synthesis of CH4930808 (1), a novel anti-hepatitis C virus agent. While pursuing improved productivity using many through-process strategies, we conducted scrupulous impurity control. Finally, we successfully developed a practical and scalable process for the synthesis of (1-1.5Na center dot 2.5H(2)O), by which we prepared 3.28 kg of the active pharmaceutical ingredient for clinical studies.

引用

页码：236 / 240

页数：5

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