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1. 发明授权

US5756775A Process to make .alpha.,.alpha.-difluoro-.beta.-hydroxyl thiol esters 失效
标题翻译：制备α，α-二氟-β-羟基硫醇酯的方法
公开(公告)号：US5756775A
公开(公告)日：1998-05-26
申请号：US762622
申请日：1996-12-09
申请人： John A. Weigel
发明人： John A. Weigel
IPC分类号： C07C327/22 , C07D307/33 , C07D317/30 , C07H13/08 , C07H19/06 , C07C327/00 , C07D317/00 , C07D317/44
CPC分类号： C07D307/33 , C07C327/22 , C07D317/30 , C07H13/08 , C07H19/06 , C07C2101/16
摘要： A process to make .alpha.,.alpha.-difluoro-.beta.-hydroxy thiol esters of formula (IIIA) ##STR1## comprising reacting a difluoroethanethioate of formula (IVA) ##STR2## with a second reactant selected from the group consisting of aldehydes, ketones, acid halides and esters; in a solvent and in the presence of a strong base; with the proviso that the process is conducted in the absence of a catalyst and in the absence of a silyl containing compound. These thiol esters are useful as intermediates in organic syntheses of pharmaceutical products.
摘要翻译：制备式（IIIA）的α，α-二氟-β-羟基硫羟酸酯（IIIA）的方法，包括使式（IVA）的二氟乙硫乙酸酯（IVA）与选自以下的第二反应物的醛，酮，酰卤和酯; 在溶剂中并在强碱的存在下进行; 条件是该方法在不存在催化剂的情况下和在不存在含甲硅烷基的化合物的情况下进行。这些硫醇酯可用作药物有机合成中的中间体。

2. 发明授权

US5912366A .alpha., .alpha.-Difluoro-.beta.-hydroxy thiol esters and their synthesis 失效
标题翻译： α，α-二氟-β-羟基硫醇酯及其合成
公开(公告)号：US5912366A
公开(公告)日：1999-06-15
申请号：US10438
申请日：1998-01-22
申请人： John A. Weigel
发明人： John A. Weigel
IPC分类号： C07C327/22 , C07D307/33 , C07D317/30 , C07H13/08 , C07H19/06 , C07D317/00 , C07C327/00 , C07D317/44
CPC分类号： C07D307/33 , C07C327/22 , C07D317/30 , C07H13/08 , C07H19/06 , C07C2101/16
摘要： .alpha.,.alpha.-Difluoro-.beta.-hydroxy thiol esters of Formula (III): ##STR1## wherein: R.sup.c and R.sup.d are independently selected from the group consisting of H, C.sub.1 -C.sub.6 alkyl, substituted C.sub.1 -C.sub.6 alkyl, S-tert-butyl difluorothioacet-2-yl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.3 -C.sub.8 cycloalkenyl, substituted C.sub.3 -C.sub.8 cycloalkyl, substituted C.sub.3 -C.sub.8 cycloalkenyl, aryl, substituted aryl, C.sub.6 -C.sub.10 fused aromatic rings, and substituted C.sub.6 -C.sub.10 fused aromatic rings; orR.sup.c and R.sup.d together make up a ring selected from the group consisting of C.sub.3 -C.sub.8 cycloalkyl, C.sub.3 -C.sub.8 cycloalkenyl, substituted C.sub.3 -C.sub.8 cycloalkyl and substituted C.sub.3 -C.sub.8 cycloalkenyl;R.sup.e is selected from the group consisting of C.sub.1 -C.sub.10 alkyl, substituted C.sub.1 -C.sub.10 alkyl, aryl, substituted aryl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.3 -C.sub.8 cycloalkenyl, substituted C.sub.3 -C.sub.8 cycloalkyl and substituted C.sub.3 -C.sub.8 cycloalkenyl, C.sub.6 -C.sub.10 fused aromatic rings, and substituted C.sub.6 -C.sub.10 fused aromatic rings; are described and claimed. Also described and claimed is a process to make these thiol esters. These thiol esters are useful as intermediates in organic syntheses of pharmaceutical products.
摘要翻译：式（III）的α-二氟-β-羟基硫醇酯：其中：R c和R d独立地选自H，C 1 -C 6烷基，取代的C 1 -C 6烷基，S-叔丁基二氟硫代乙酸酯， C 3 -C 8环烷基，C 3 -C 8环烯基，取代的C 3 -C 8环烷基，取代的C 3 -C 8环烯基，芳基，取代的芳基，C 6 -C 10稠合芳环和取代的C 6 -C 10稠合芳环; 或Rc和Rd一起构成选自C 3 -C 8环烷基，C 3 -C 8环烯基，取代的C 3 -C 8环烷基和取代的C 3 -C 8环烯基的环; R 6选自C 1 -C 10烷基，取代的C 1 -C 10烷基，芳基，取代的芳基，C 3 -C 8环烷基，C 3 -C 8环烯基，取代的C 3 -C 8环烷基和取代的C 3 -C 8环烯基，C 6 -C 10稠合芳环和取代的C 6 -C 10稠合芳环; 被描述和要求保护。还描述和要求保护的是制备这些硫醇酯的方法。这些硫醇酯可用作药物有机合成中的中间体。

3. 发明授权

US6001994A Process for making gemcitabine hydrochloride 失效
标题翻译：制造盐酸吉西他滨的方法
公开(公告)号：US6001994A
公开(公告)日：1999-12-14
申请号：US209398
申请日：1998-12-10
申请人： John A. Weigel
发明人： John A. Weigel
IPC分类号： C07C327/22 , C07D307/33 , C07D317/30 , C07H13/08 , C07H19/06 , C07H19/00 , C07C327/00
CPC分类号： C07D307/33 , C07C327/22 , C07D317/30 , C07H13/08 , C07H19/06 , C07C2101/16
摘要： An improved process to make gemcitabine hydrocrhloride, the improvement consisting essentially of making the lactone intermediate, 2-deoxy-2,2-difluoro-D-erythro-pentafuranose-1 ulose-3,5-dibenzoate: ##STR1## from D-erythro-2-Deoxy-2,2-difluoro 4,5-O-(1-ethylpropyl)-idene) pentoic acid tert Butyl ester wherein, the D-erythro-2-deoxy-2,2 difluoro-4,5-O-(1-ethylproyl)-ideno) pentoic acid tert-Butyl ester is prepared by the process of reacting S-tert-butyl difluoroethane thioate with 2,3-O (1-ethylpropylidene)-D-glyceraldehyde, in a solvent and in the presence of a strong base; with the proviso that the process is conducted in the absence of a catalyst and in the absence of a silyl containing compound.
摘要翻译：制备吉西他滨加氢氯化物的改进方法，其改进基本上由制备内酯中间体，2-脱氧-2,2-二氟-D-赤藓 - 五氟尿嘧啶-1肟基-3,5-二苯甲酸酯：从D-赤式-2- 脱氧-2,2-二氟4,5-（1-乙基丙基） - 亚基）戊酸叔丁酯其中，D-赤式-2-脱氧-2,2-二氟-4,5-O-（1 - 乙基丙基） - 异诺烯）戊酸叔丁酯通过使S-叔丁基二氟乙烷硫酸酯与2,3-O（1-乙基亚丙基）-D-甘油醛在溶剂中和在强大的基地; 条件是该方法在不存在催化剂的情况下和在不存在含甲硅烷基的化合物的情况下进行。

4. 发明授权

US5428176A Process for preparing 2,2-difluoroketene silyl O,S-acetals and .alpha.,.alpha.-difluoro-.beta.-silyloxy-1,3-dioxolane-4-propanoic acid O,S-esters 失效
标题翻译：制备2,2-二氟乙烯甲硅烷基O，S-缩醛和α，α-二氟-β-甲硅烷氧基-1,3-二氧戊环-4-丙酸O，S-酯的方法
公开(公告)号：US5428176A
公开(公告)日：1995-06-27
申请号：US227820
申请日：1994-04-14
申请人： John A. Weigel
发明人： John A. Weigel
IPC分类号： C07F7/18 , C07D317/18 , C07F7/04
CPC分类号： C07F7/188 , C07F7/1852 , C07F7/1892
摘要： Processes for preparing 2,2-difluoroketene silyl O,S-acetals and .alpha.,.alpha.-difluoro-.beta.-silyloxy-1,3-dioxolane-4-propanoic acid O,S-esters.
摘要翻译：制备2,2-二氟乙烯甲硅烷基O，S-缩醛和α，α-二氟-β-甲硅烷氧基-1,3-二氧戊环-4-丙酸O，S-酯的方法。

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