- Method of manufacturing sulfonylhalides unsatd. alkyl
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PROBLEM TO BE SOLVED: To provide a production method capable of industrially simply and efficiently providing unsaturated alkyl halides useful as functional compounds, pharmaceuticals, agrochemicals or intermediates thereof.SOLUTION: Vinyl chloride and a Grignard reagent derived from a dihaloalkane represented by the specified general formula (1), where Xand Xeach independently represent Cl, Br or I and n represents an integer from 4 to 12, are reacted in the presence of an iron compound to produce unsaturated alkyl halides represented by the specified general formula (2), where Xrepresents Cl, Br or I and n represents an integer from 4 to 12.
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Paragraph 0035; 0036; 0037
(2017/03/08)
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- Efficient synthesis of (S)-2-(cyclopentyloxycarbonyl)-amino-8-nonenoic acid: Key building block for BILN 2061, an HCV NS3 protease inhibitor
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A new procedure for the practical synthesis of (S)-2-(cyclopen- tyloxycarbonyl)amino-8-nonenoic acid, a key building block for BILN 2061, an HCV NS3 protease inhibitor, has been developed. The key step features a kinetic resolution of racemic 2-acetylamino-8-nonenoic acid with acylase I. In addition, the undesired (R)-2-acetylamino-8-nonenoic acid was recycled after racemization. The procedure was implemented for the production of (S)-2-(cyclopentyloxycarbonyl)amino-8-nonenoic acid on pilot-plant scale.
- Wang, Xiao-Jun,Zhang, Li,Smith-Keenan, Lana L.,Houpis, Ioannis N.,Farina, Vittorio
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