Development of an Efficient, Scalable Route for the Preparation of a Novel Insulin-Like Growth Factor-1 Receptor Modulator

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• 作者：CH Vinod Kumar ; Santosh Kavitake ; Sythana Suresh Kumar ; Philip Cornwall ; Mithun Ashok ; Sagar Bhagat ; Sulur G. Manjunatha ; Sudhir Nambiar
• 刊名：Organic Process Research & Development
• 出版年：2012
• 出版时间：August 17, 2012
• 年：2012
• 卷：16
• 期：8
• 页码：1416-1421
• 全文大小：290K
• 年卷期：v.16,no.8(August 17, 2012)
• ISSN：1520-586X

文摘

A chromatography-free and efficient synthesis of insulin-like growth factor-1 receptor (IGF-1R) modulator is reported. Herein we describe an improved synthesis for the target compound, which features facile introduction of a novel pyrrolidinyl-pyrimidyl isoxazole 8, via in situ sulfone displacement by fluorine. The overall process consists of six chemical steps and five isolations, with introduction of the expensive triheterocyclic unit 8 towards the end of the synthesis.