CAS: 60468-36-2; 2-Chloro-2',5'-Difluoroacetophenone

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CAS号540-36-3 1,4-二氟苯 | CAS号79-04-9 氯乙酰氯

2,5-二氟苯乙酮置于n-氯代丁二酰亚胺,对甲苯磺酸体系中,化学反应生成 2-氯-2`,5`-二氟苯乙酮
参考文献:级联三硫自由基(s 3 •-)加成/电子脱甲苯磺酸合成1,2,3-噻二唑和异噻唑
标题:级联三硫自由基(s 3 •-)加成/电子脱甲苯磺酸合成1,2,3-噻二唑和异噻唑
摘要:已经开发了三硫自由基阴离子(s 3 •-)与原位形成的偶氮烯烃和α,β-过饱和的n-磺酰亚胺类化合物介导的反应,用于构建1,2,3-噻二唑和异噻唑.s 3 •-是由dmf中的硫化钾原位反应生成的.这两种方法提供了一种新的,安全的和简单的方法来以高收率构建4-取代的1,2,3-噻二唑,5-取代的1,2,3-噻二唑和异噻唑.反应包括在温和条件下通过s 3 •加成形成新的c-s和n-s键和电子脱甲苯基化反应.
DOI:10.1021/acs.Joc.8B01450

专利信息

专利号:US-9481680-B2
优先权日:2014-03-20
标题 :Process for the preparation of key intermediates of omarigliptin
发明人：DE LUCCHI OTTORINO; ROSSO ENRICO; ZARAMELLA SIMONE; TARTAGGIA STEFANO
权利人:F I S —FABBRICA ITALIANA SINTETICI S P A; F I S —FABBRICA ITALIANA SINTETICI S P A
摘要:An improved process for the preparation of a key intermediate for the synthesis of the active ingredient Omarigliptin is provided. The key intermediate is a compound having the following formula (I) n nwherein R 1 is propargyl or allyl group and P is an amine protecting group. The compound of formula (I) is prepared by converting a compound of formula (IV)n n nby an amination reaction to a compound of formula (III),n n nwhich is then protected to provide a compound of formula (II),n n nwhich is then alkylated to provide the compound of formula (I).