首页> 外国专利> METHOD FOR PRODUCING EPOTHYLONE DERIVATIVES, NEW EPOTHYLON DERIVATIVES, AND ALSO NEW INTERMEDIATE COMPOUNDS FOR IMPLEMENTATION OF THE METHOD AND METHODS FOR PRODUCING THEM

METHOD FOR PRODUCING EPOTHYLONE DERIVATIVES, NEW EPOTHYLON DERIVATIVES, AND ALSO NEW INTERMEDIATE COMPOUNDS FOR IMPLEMENTATION OF THE METHOD AND METHODS FOR PRODUCING THEM

机译:制备乙酮衍生物,新的乙缩醛衍生物的方法以及用于实施该方法的新中间体化合物及其制备方法

摘要

1. The compounds of formula 9! ! where R1 is methyl, a R2 is unsubstituted or substituted aryl, and salts with metal cations. ! 2. The compounds of formula 9! ! where R1 is methyl, a R2 is unsubstituted or substituted phenyl, and salts with metal cations. ! 3. The compounds of formula 3! ! where R2 has the meanings given in the definition of formula 9.! 4. A method of obtaining compounds of formula 3, characterized in that the compound of formula 1,! where R2 has the meanings indicated above, and the mesyl group in all subsequent reactions is replaced by tosyl and a similar group, interacts with the sultam derivative of formula 2 in all subsequent stages of the reaction, for example,! ! in the reaction of selective aldol condensation in the presence of a Lewis acid and with the addition of a base in an inert solvent at a reduced temperature from -50 ° C to -100 ° C, and then at an elevated temperature from -20 ° C to 20 ° C, with the formation of a compound of formula 3 .! 5. The compounds of formula 4! ! where R2 has the meanings indicated above. ! 6. A method of obtaining compounds of formula 4, characterized in that the compound of formula 3! ! interacts with the silyl ether forming compound at a temperature of from -70 ° C to 25 ° C in the presence of 2,6-lutidine to form the above compound of formula 4.! 7. The compounds of formula 5! ! where R2 has the meanings indicated above. ! 8. The method of obtaining new compounds of formula 5, characterized in that in the compounds of formula 4! ! by treatment with TBAOH / H2O2 in DME or LiO2H in THF / MeOH / H2O, the chiral auxiliary group is cleaved to form a carboxylic acid, i.e. compounds of formula 5.! 9. The compounds of formula 6! ! where R2 has the meanings indicated above. ! 10. The method of obtaining new compounds of formula 6,
机译:1.式9的化合物! !其中R1是甲基,R2是未取代或取代的芳基,以及与金属阳离子的盐。 ! 2.式9的化合物! !其中R1是甲基,R2是未取代或取代的苯基,以及与金属阳离子的盐。 ! 3.式3的化合物! !其中R2具有在式9的定义中给出的含义! 4.获得式3的化合物的方法,其特征在于式1的化合物!其中R 2具有上述含义,并且在所有后续反应中的甲磺酰基均被甲苯磺酰基和类似的基团取代,在反应的所有后续阶段均与式2的sultam衍生物相互作用,例如! !在路易斯酸存在下,在惰性溶剂中加入碱,在-50°C至-100°C的降低温度下,然后在-20°C的高温下,选择性醛醇缩合反应℃至20℃,形成式3化合物。 5.式4的化合物! !其中R2具有上述含义。 ! 6.获得式4的化合物的方法,其特征在于式3的化合物! !在2,6-二甲基吡啶存在下,在-70°C至25°C的温度下与形成甲硅烷基醚的化合物相互作用,形成上述式4的化合物! 7.式5的化合物! !其中R2具有上述含义。 ! 8.获得新的式5化合物的方法,其特征在于在式4的化合物中! !通过在DME中用TBAOH / H 2 O 2或在THF / MeOH / H 2 O中用LiO 2 H处理,手性辅助基团被裂解形成羧酸,即式5的化合物。 9.式6的化合物! !其中R2具有上述含义。 ! 10.获得式6的新化合物的方法

著录项

相似文献

  • 专利
  • 外文文献
  • 中文文献
获取专利

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号