公开(公告)号：US3870710A

公开(公告)日：1975-03-11

申请号：US33041173

申请日：1973-02-07

Applicant: ROUSSEL UCLAF

Inventor： MARTEL JACQUES ,  TOROMANOFF EDMOND ,  BUENDIA JEAN

IPC: C07C59/90 ,  C07C405/00 ,  C07D303/42 ,  C07D309/12 ,  C07C69/74 ,  C07D7/04

CPC classification number: C07C59/90 ,  C07C405/00 ,  C07D303/42 ,  C07D309/12 ,  Y10S514/866

Abstract: WHEREIN R is selected from the group consisting of hydrogen and alkyl of 1 to 7 carbon atoms, R1 is selected from the group consisting of hydrogen and carbalkoxy of 1 to 7 alkyl carbon atoms, R2 is selected from the group consisting of hydrogen, carboxy and carbalkoxy of 1 to 7 alkyl carbon atoms, R3 is selected from the group consisting of hydrogen and Alpha tetrahydropyranyl, m is 3,4 or 5 and n is 2,3 or 4 with the proviso that when R1 is carbalkoxy, R is alkyl of 1 to 7 carbon atoms, R2 is hydrogen and R3 is Alpha -tetrahydro pyranyl; when R2 is carbalkoxy, R is alkyl of 1 to 7 carbon atoms, R1 is hydrogen and R3 is Alpha -tetrahydropyranyl and when R2 is carboxy, R and R1 are hydrogen and R3 is Alpha tetrahydropyranyl, which possess the physiological activity of prostaglandins, and salts thereof when R, R1, R2 and R3 are hydrogen, with non-toxic, pharmaceutically acceptable bases and their preparation.

Novel prostanoic acid derivatives of the formula

Abstract translation: 式WHEREIN R的新型前列腺烷酸衍生物选自氢和1至7个碳原子的烷基，R 1选自氢和1至7个烷基碳原子的烷氧基，R2选自 由1至7个碳原子的氢，羧基和烷氧基组成的基团，R 3选自氢和α-四氢吡喃基，m为3,4或5，n为2,3或4，条件是当 R1是烷氧基，R是1至7个碳原子的烷基，R2是氢，R3是α-四氢吡喃基; 当R 2为烷氧基时，R为1至7个碳原子的烷基，R 1为氢，R 3为α-四氢吡喃基，当R 2为羧基时，R 1和R 1为氢，R 3为具有前列腺素生理活性的α-四氢吡喃基， 当R，R 1，R 2和R 3为氢时，其盐为无毒，药学上可接受的碱及其制备。

公开(公告)号：US3694472A

公开(公告)日：1972-09-26

申请号：US3694472D

申请日：1970-05-12

Applicant: ROUSSEL UCLAF

Inventor： MARTEL JACQUES ,  BUENDIA JEAN

IPC: C07C62/16 ,  C07C69/74

CPC classification number: C07C62/16

Abstract: BY REACTING 3,3-DIMETHYL-2-FORMYL-1-CYCLOPROPANECARBOXYLIC (1R, 2R) acid or a salt thereof with methyl propionate under anhydrous basic conditions.

A novel process for the preparation of 3,3-dimethyl-2-(2''methoxycarbonyl-trans 1''-propenyl)-1-cyclopropane carboxylic (1R, 2R) acid or d-trans pyrethric (1R,2R) acid of the formula

Abstract translation: 制备3,3-二甲基-2-（2'-甲氧基羰基 - 反式-1'-丙烯基）-1-环丙烷羧酸（1R，2R）酸或d-反式除虫菊酸（1R，2R）酸的新方法 通过在无水碱性条件下将3,3-二甲基-2-甲基-1-环丙基碳酰氧基（1R，2R）酸或其盐与丙酸甲酯反应。

公开(公告)号：US3870711A

公开(公告)日：1975-03-11

申请号：US40070973

申请日：1973-09-26

Applicant: ROUSSEL UCLAF

Inventor： MARTEL JACQUES ,  BUENDIA JEAN ,  TOROMANOFF EDMOND

IPC: C07C405/00 ,  C07D303/42 ,  C07D309/12 ,  C07D521/00 ,  C07D7/02

CPC classification number: C07D231/12 ,  C07C405/00 ,  C07D233/56 ,  C07D249/08 ,  C07D303/42 ,  C07D309/12

Abstract: Novel intermediates formed in the process for the preparation of derivatives of prostanoic acids of the prostaglandin A2 (PGA2) group of the formula

WHEREIN R is selected from the group consisting of hydrogen and lower alkyl, n is a whole number of 2,3 or 4 and m is a whole number of 3,4 or 5 and to novel intermediates produced in the said process.

Abstract translation: 在制备式WHEREIN R的前列腺素A2（PGA2）基的前列腺酸衍生物的方法中形成的新型中间体选自氢和低级烷基，n是整数2,3或4 并且m是3,4或5的整数，并且在所述方法中产生的新的中间体。

公开(公告)号：US3862160A

公开(公告)日：1975-01-21

申请号：US38206173

申请日：1973-07-24

Applicant: ROUSSEL UCLAF

Inventor： MARTEL JACQUES ,  BUENDIA JEAN ,  COSTEROUSSE GERMAIN

IPC: C07D209/16 ,  C07D309/30 ,  C07D461/00 ,  C07D471/04 ,  C07D471/14 ,  C07D27/54

CPC classification number: C07D471/04 ,  C07D209/16 ,  C07D309/30 ,  C07D461/00 ,  C07D471/14

Abstract: The preparation of derivatives of 1,2,3,4-tetrahydro-9H-pyrido (3,4-b) indole is described. In particular the preparation of acrylic esters of Beta -(3''-hydroxypropyl)-1,2,3,4-tetrahydro9H-pyrido (3,4-b) indole is shown to proceed from the oxidation of a 2-alkyloxy-3-hydroxytetrahydropyran to its 2-alkyloxy-3oxotetrahydropyran derivative. The Wittig condensation is used to effect the reaction of this ketone with a phosphonoacetic ester giving rise to the carbalkoxy methylenic-substitution product, 2alkyloxy-3-(1''-alkoxycarbonyl)methylidenetetrahydropyran. After acid hydrolysis of the 2-alkyloxy group, condensation is carried out with tryptamine resulting in the desired indole derivatives. Such compounds can be used in the facile preparation of alkaloids of the eburnamonie family.

Abstract translation: 描述了1,2,3,4-四氢-9H-吡啶并[3,4-b]吲哚衍生物的制备。 具体地说，β-（3'-羟丙基）-1,2,3,4-四氢-9H-吡啶并[3,4-b]吲哚的丙烯酸酯的制备显示出从2-烷氧基 -3-羟基四氢吡喃与其2-烷氧基-3-氧代四氢吡喃衍生物。 维t嗪缩合用于使该酮与一种膦酰基乙酸酯反应，生成2-烷氧基-3-（1'-烷氧基羰基）亚甲基四氢吡喃的烷氧基亚甲基取代产物。 在2-烷氧基酸水解后，用色胺进行缩合，产生所需的吲哚衍生物。 这些化合物可用于易燃鳗ie族家族生物碱的制备。