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1. 发明授权

US4870199A Processes for the synthesis of diprotected R[R*,S*]-3,5-dihydroxy-6-oxohexanoate esters 失效
标题翻译：合成二保护R [R *，S *] - 3,5-二羟基-6-氧代己酸酯的方法
公开(公告)号：US4870199A
公开(公告)日：1989-09-26
申请号：US166594
申请日：1988-03-10
申请人： Kau-Ming Chen , Goetz E. Hardtmann , Prasad K. Kapa , George T. Lee , Jerome Linder , Sompong Wattanasin
发明人： Kau-Ming Chen , Goetz E. Hardtmann , Prasad K. Kapa , George T. Lee , Jerome Linder , Sompong Wattanasin
IPC分类号： C07D209/18 , C07D233/54 , C07F7/18
CPC分类号： C07D233/64 , C07D209/18 , C07F7/1852 , Y02P20/55
摘要： Process for the synthesis of compounds of the formula ##STR1## in R[R*,S*] enantiomeric form, wherein each P.sub.1 is independently an hydroxy group-protecting group, andR.sub.2z is C.sub.1-4 alkyl, benzyl or allyl,comprising, as a key step when R.sub.2z is R.sub.2x, the reaction of the compound of the formula ##STR2## in (S) enantiomeric form with a compound of the formulaMg.sup. .circle.+2 (.sup..crclbar. OOC--CH.sub.2 --COOR.sub.2x).sub.2to obtain a compound of the formula ##STR3## in (S) enantiomeric form, and, as a key step when R.sub.2z is R.sub.2y, the reaction of a compound of the formula ##STR4## in (S) enantioimeric form with a compound of the formulaLi.sup..sym..crclbar. CH.sub.2 --COOR.sub.2yto obtain a compound of the formula ##STR5## in (S) enantiomeric form, wherein R.sub.2x is primary or secondary C.sub.1-4 alkyl, benzyl or allyl,R.sub.2y is C.sub.1-4 alkyl not containing an asymmetric carbon atom, andR.sub.3 ' is methyl or ethyl,processes for the synthesis of compounds of the formula ##STR6## comprising reacting a compound of the formula ##STR7## with the reaction product of a strong base and a compound of the formula ##STR8## optionally followed by, when R.sub.2z is allyl, cleavage of the allyl and P.sub.1 groups to obtain the corresponding compound of the formula ##STR9## wherein each R.sub.7 is methyl or ethyl,R is as defined in the specification, and eachP.sub.1 independently and R.sub.2z are as defined above, andthe compounds of the formula ##STR10## wherein R and each R.sub.7 are as defined above.
摘要翻译：用于合成R [R *，S *]对映体形式的式“IMAGE”的化合物的方法，其中每个P1独立地是羟基保护基，R2z是C1-4烷基，苄基或烯丙基，包括作为 R2z为R2x时的关键步骤，式（S）对映异构形式的式（IMA）化合物与式Mg＆cir＆+2（（ - ）OOC-CH2-COOR2x）2的化合物的反应，得到化合物式（S）对映体形式的式（IMAGE）式中，作为R2z为R2y的关键步骤，式（S）对映异构体形式的式“IMAGE”的化合物与式Li ）（ - ）CH2-COOR2y，得到（S）对映异构体形式的下式的化合物，其中R2x是伯或仲C 1-4烷基，苄基或烯丙基，R2y是不含不对称碳原子的C 1-4烷基，并且R 3'是甲基或乙基，用于合成式IMA化合物的方法包括使式IMA的化合物与强碱的反应产物 da化合物，其中当R 2z是烯丙基时，烯丙基和P1基团裂解，得到相应的式“IMAGE”化合物，其中每个R 7是甲基或乙基，R如说明书中所定义，每个P1独立地和R2z如上所定义，并且式“IMAGE”的化合物其中R和每个R 7如上所定义。

2. 发明授权

US5189164A Processes for the synthesis of syn-(E)-3,5-dihydroxy-7-substituted hept-6-enoic and heptanoic acids and derivatives and intermediates thereof 失效
标题翻译：合成顺式（E）-3,5-二羟基-7-取代的庚-6-烯酸和庚酸及其衍生物及其中间体的方法
公开(公告)号：US5189164A
公开(公告)日：1993-02-23
申请号：US482433
申请日：1990-02-20
申请人： Prasad K. Kapa , Kau-Ming Chen
发明人： Prasad K. Kapa , Kau-Ming Chen
IPC分类号： C07C51/367 , C07D209/12 , C07D209/24 , C07D233/54
CPC分类号： C07D233/64 , C07C51/367 , C07D209/12 , C07D209/24
摘要： A process for synthesizing syn-(E)-3,5-dihydroxy-7-substituted hept-6-enoic and heptanoic acids and derivatives and intermediates thereof from the corresponding keto-hydroxy compounds, which process comprises: providing a reaction medium comprising sodium borohydride and an alkoxydialkylborane compound; treating the keto-hydroxy compound with said reaction medium under conditions wherein a cyclic boronate ester is formed; and cleaving the cyclic boronate ester to obtain the dihydroxy product.The product compounds, or derivatives thereof, are useful as anti-atherosclerotic agents.
摘要翻译：从相应的酮 - 羟基化合物合成顺式 - （E）-3,5-二羟基-7-取代的庚-6-烯酸和庚酸及其衍生物及其中间体的方法，该方法包括：提供包含钠硼氢化物和烷氧基二烷基硼烷化合物; 在形成环状硼酸酯的条件下用所述反应介质处理酮 - 羟基化合物; 并切割环状硼酸酯以获得二羟基产物。产物化合物或其衍生物可用作抗动脉粥样硬化剂。

3. 发明授权

US4847384A Process for the preparation of certain nitrogen-containing mono- and bicyclic ace inhibitors, and novel intermediates useful therefor 失效
标题翻译：用于制备某些含氮单环和双环ace抑制剂的方法，以及可用于其的新型中间体
公开(公告)号：US4847384A
公开(公告)日：1989-07-11
申请号：US24959
申请日：1987-03-12
申请人： Prasad K. Kapa , Kau-Ming Chen
发明人： Prasad K. Kapa , Kau-Ming Chen
IPC分类号： C07K5/02
CPC分类号： C07K5/0222
摘要： An improved process for preparing certain nitrogen-containing mono- and bicyclic ACE inhibitors comprising reacting an .alpha.-alkyl amino acid with a disulfide compound to form a thioester intermediate, which intermediate is then amidated with a mono- or bicyclic amino acid. The invention also relates to the novel thioester intermediates prepared by the first step of the process.
摘要翻译：一种用于制备某些含氮单环和双环ACE抑制剂的改进方法，包括使α-烷基氨基酸与二硫化物化合物反应形成硫酯中间体，然后将该中间体与单环或双环氨基酸酰胺化。本发明还涉及通过该方法的第一步制备的新的硫酯中间体。

4. 发明授权

US07151179B2 Process for the preparation of 7-alkyl-10-hydroxy-20(S)-camptothecin 有权
标题翻译：制备7-烷基-10-羟基-20（S） - 喜树碱的方法
公开(公告)号：US07151179B2
公开(公告)日：2006-12-19
申请号：US10844225
申请日：2004-05-12
申请人： Chien-Hsing Lin , Yung-Fa Chen , Kau-Ming Chen
发明人： Chien-Hsing Lin , Yung-Fa Chen , Kau-Ming Chen
IPC分类号： C07D405/14
CPC分类号： C07D491/22
摘要： The key intermediate in any synthesis of Irinotecan is 7-ethyl-10-hydroxy-20(S)-camptothecin. A process for the efficient synthesis of this intermediate is demonstrated proceeding through readily available 20(S)-camptothecin. Various other tecan compounds may be made by use of corresponding 7-alkyl-10-hydroxy-20(S)-camptothecin intermediates.
摘要翻译：任何伊立替康合成中的关键中间体是7-乙基-10-羟基-20（S） - 喜树碱。证明通过容易获得的20（S） - 喜树碱进行有效合成该中间体的方法。可以通过使用相应的7-烷基-10-羟基-20（S） - 喜树碱中间体制备各种其它tecan化合物。

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