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PROCESS FOR PRODUCING BICYCLIC LACTONE DERIVATIVES UTILIZABLE AS INTERMEDIATES IN THE SYNTHESIS OF PROSTAGLANDINES

机译:生产可作为中间体合成前列腺素的双环内酯衍生物的方法

摘要

The invention 1s concerned with a novel process for producing compounds of formula 1 I wherein R3 and R4 are the same or different and each represent hydrogen or a lower alkanoyl group whlich is unsubstituted or is substituted by one, two or three halogen atoms, or R3 and R4 together form a qroup R5-?-R6 wherelin R5 and R6 are the same or different and each represent hydrogen or a methyl or phenyl group, with the proviso that when one of R5 and R6 is phenyl the other is hydrogen. The compounds of formula I are obtained by reacting a lactone of formula II II with formaldehyde or a polymer of formaldehyde in the procence of a strong acid, followed, if necessary, by reaction with a compound of formula R5COR6 or R5CHO or an acetal thereof. The compounds of formula I are useful lntermediates in Corey's synthesis of prostaglandins and those compounds in which R3 and R4 form a group ,5-?-R are novel.
机译:本发明涉及一种制备式I化合物的新方法,其中R 3和R 4相同或不同,并且各自代表氢或低级烷酰基,其中未被取代或被一个,两个或三个卤素原子取代,或R 3 R5和R4一起形成一个基团R5-β-R6,其中R5和R6相同或不同,分别代表氢或甲基或苯基,条件是当R5和R6之一为苯基时,另一个为氢。式I化合物是通过使式II II的内酯与甲醛或甲醛的聚合物在强酸中反应,然后根据需要与式R 5 COR 6或R 5 CHO的化合物或其缩醛反应而获得的。式I化合物在Corey的前列腺素合成中是有用的中间体,其中R 3和R 4形成基团,5-α-R的那些化合物是新颖的。

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