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1. 发明申请

WO8704427A3 PROSTAGLANDIN SYNTHESIS 审中-公开
标题翻译：前列腺素合成
公开(公告)号：WO8704427A3
公开(公告)日：1987-12-03
申请号：PCT/GB8700019
申请日：1987-01-15
申请人： NAT RES DEV
发明人： JONES ROBERT LESLIE , WILSON NORMAN HAPPER
IPC分类号： C07C69/03 , C07B61/00 , C07C51/00 , C07C51/353 , C07C59/125 , C07C59/205 , C07C59/80 , C07C67/00 , C07C67/347 , C07C231/00 , C07C231/02 , C07C231/12 , C07C235/82 , C07C325/00 , C07C327/24 , C07C405/00 , C07D493/08 , C07C69/708
CPC分类号： C07D493/08 , C07C59/80 , C07C405/0091
摘要： A process for the preparation of a compound of formula (I), wherein X and X' each represents hydrogen or together represent a bridging group -CH2-, -CH2-CH2- or -O-; R1 is a 6-carboxyhex-2-enyl group or a modification thereof in which the group is altered by one, or an appropriate combination of two or more, of the following: (a) alteration of the position of the double bond, with the proviso that in the modified group the double bond is not in the alpha-beta position relative to the ring; (b) reduction of the double bond; (c) alteration of the chain length through a decrease of one or two methylene groups or an increase of one to six methylene groups; (d) replacement of one or two methylene groups each separately by an oxygen or sulphur atom, with the proviso that in the modified group no oxygen or sulphur atom is in an alpha position relative to either a doubly bonded carbon atom or to the carboxy group or a derivative thereof and that at least 2 carbon atomes separate any pair of oxygen and/or sulphur atoms; and (e) formation of an amide, ester or salt derivative of the carboxy group; R2 is an aliphatic hydrocarbon group or an aliphatic hydrocarbon group substituted by an aromatic group directly or through an oxygen or sulphur atom; and R3, R4, R5 and R6 are each hydrogen, or R3 and R4 together and/or R5 and R6 together represent the second bond of a carbon-carbon double bond; comprises effecting a Diels Alder reaction between a diene of formula (II) and a dienophile of formula (III), wherein X, X' and R2 are as defined for (I); Y is R1 or a precursor therefor in which a double bond is present and/or the terminal group is in different form, either being a free carboxy group rather than the carboxy group derivative present in R1 or being a carboxy group derivative rather than the free carboxy group present in R1; and R and R' are either each hydrogen or together represent the third bond of a carbon-carbon triple bond; and where appropriate thereafter, in either order, reducing the double bond or bonds in the ring of the Diels Alder adduct and/or converting the group Y to the group R1. The compounds prepared by this process are of value as intermediates for the preparation of biologically active compounds.
摘要翻译：制备式（I）化合物的方法，其中X和X'各自代表氢或一起代表桥基-CH 2 - ， - CH 2 -CH 2 - 或-O-; R1是6-羧基己-2-烯基或其修饰，其中该基团被以下的一个或两个或更多个的适当组合改变：（a）改变双键的位置，与条件是在修饰基团中双键不在相对于环的α-β位; （b）减少双键; （c）通过减少一个或两个亚甲基或增加一个至六个亚甲基而改变链长; （d）分别用氧或硫原子分别置换一个或两个亚甲基，条件是在修饰基团中氧或硫原子相对于双键碳原子或羧基处于α位或其衍生物，并且至少2个碳原子分离任何一对氧原子和/或硫原子; 和（e）形成羧基的酰胺，酯或盐衍生物; R2是直接或通过氧或硫原子被芳基取代的脂族烃基或脂族烃基; 并且R3，R4，R5和R6各自为氢，或者R3和R4一起和/或R5和R6一起表示碳 - 碳双键的第二键; 包括在式（II）的二烯与式（III）的亲二烯体之间进行狄尔斯阿尔德反应，其中X，X'和R2如对（I）所定义; Y是R 1或其中存在双键的前体和/或末端基团是不同形式，或者是游离羧基而不是存在于R 1中的羧基衍生物或者是羧基衍生物而不是游离的存在于R1中的羧基; 并且R和R'各自为氢或一起表示碳 - 碳三键的第三键; 然后以任意次序，减少Diels Alder加合物的环中的双键或键和/或将基团Y转化为基团R1。通过该方法制备的化合物作为制备生物活性化合物的中间体是有价值的。

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