Process Development and Scale-Up of AZD7545, a PDK Inhibitor

被引：18

作者：

Patel, Bharti ^{[1
]}

Firkin, Catherine R. ^{[1
]}

Snape, Evan W. ^{[1
]}

Jenkin, Shelley L. ^{[1
]}

Brown, David ^{[1
]}

Chaffey, Julian G. K. ^{[1
]}

Hopes, Philip A. ^{[1
]}

Reens, Carl D. ^{[2
]}

Butters, Mike ^{[1
]}

Moseley, Jonathan D. ^{[1
]}

机构：

[1] AstraZeneca, Avlon Works, Proc Res & Dev, Bristol BS10 7ZE, Avon, England

[2] AstraZeneca, R&D Charnwood, Dev Manufacture, Loughborough LE11 5RH, Leics, England

来源：

ORGANIC PROCESS RESEARCH & DEVELOPMENT | 2012年 / 16卷 / 03期

关键词：

TREGOE DECISION-ANALYSIS; FACILE SYNTHESIS; ACIDS; TOOL;

D O I：

10.1021/op2003419

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

A brief comparison of the early manufacturing routes to AZD7545 is given. Process development of the preferred long-term manufacturing route is reported in detail, and changes from the initial kilogram-scale route are discussed. Scale-up experience from the pilot-plant manufacture is included in the discussion of each stage. Noteworthy aspects throughout the development of AZD7545 concerned chemical hazards, mechanisms, analysis, and impurities, upon which this case study will focus.

引用

页码：447 / 460

页数：14

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