Preparation of 1-(carbamoyl)-n-(carbamoyloxy)-thioformimidates from acetoacetamides
    1.
    发明授权
    Preparation of 1-(carbamoyl)-n-(carbamoyloxy)-thioformimidates from acetoacetamides 失效
    1-乙酰氨基-N-(羧甲氧基) - 硫代丙酸酯的制备

    公开(公告)号:US3694431A

    公开(公告)日:1972-09-26

    申请号:US3694431D

    申请日:1970-09-16

    CPC classification number: C07D295/12 C07D295/20

    Abstract: 1-(Carbamoyl)-N-(carbamoyloxy)thioformimidates such as methyl 1(carbamoyl)-N-methylcarbamoyloxy)thioformimidate and methyl 1(dimethylcarbamoyl)-N-(methylcarbamoyloxy)thioformimidate are prepared by the steps of A. REACTING DIKETENE WITH AMMONIA OR AN AMINE TO OBTAIN AN ACETOACETAMIDE; B. REACTING THE PRODUCT OF (A) WITH A NITROSATING AGENT IN THE PRESENCE OF WATER OR AN ALCOHOL; C. CHLORINATING THE PRODUCT OF (B) AT A TEMPERATURE OF -10 TO 75* C.; d. reacting the product of (c) with an alkyl mercaptan and a base or with a metal salt of an alkyl mercaptan; and E. REACTING THE PRODUCT OF (D) WITH 1. A CARBAMOYL CHLORIDE IN THE PRESENCE OF A BASE; 2. PHOSGENE FOLLOWED BY REACTION WITH AN AMINE; OR 3. AN ISOCYANATE, OPTIONALLY IN THE PRESENCE OF A BASIC CATALYST; IN WATER OR ORGANIC SOLVENTS SUCH AS ACETONE, METHYLENE CHLORIDE, METHYL ETHYL KETONE, METHYL ISOBUTYL KETONE, DIMETHYLFORMAMIDE, DIMETHYLACETAMIDE, DIMETHYLSULFOXIDE, TETRAMETHYLUREA OR THEIR MIXTURES.

    Abstract translation: 通过以下步骤制备1-(氨甲酰基)-N-(氨基甲酰氧基)硫代甲亚胺酸酯如1-(氨基甲酰基)-N-甲基氨基甲酰氧基)硫代甲酰亚胺酯和1-(二甲基氨基甲酰基)-N-(甲基氨基甲酰氧基)硫代甲亚胺酸甲酯。反应DIKETENE 用氨基酸或胺获得乙酰胺; B.在水或酒精存在下,使用硝基化剂反应(A)的产物; C.在-10℃至75℃的温度下将(B)的产物进行氯化。

    CERTAIN 1,2,3,5,6,12,13a-OCTAHYDRO-12-OXO-{8 3,2,1-d,e{9 PYRIDO-{8 1,5{9 -NAPHTHYRIDINES
    9.
    发明授权
    CERTAIN 1,2,3,5,6,12,13a-OCTAHYDRO-12-OXO-{8 3,2,1-d,e{9 PYRIDO-{8 1,5{9 -NAPHTHYRIDINES 失效
    某些1,2,3,5,6,12,13a-OCTAHYDRO-12-OXO- {8 3,2,1-d,e {9 PYRIDO- {1,8,5- {9-壬基吡啶

    公开(公告)号:US3755335A

    公开(公告)日:1973-08-28

    申请号:US3755335D

    申请日:1971-03-17

    Applicant: ANVAR

    CPC classification number: C07D471/14 C07D461/00

    Abstract: The invention relates to new indole derivatives which are useful therapeutical agents. Said new derivatives are 1,2,3,5,6,12,13,13a-octahydro-12-oxo(3,2,1-d,e)-indolo-(3,2,1-i,j)-pyrido -(1,5)-naphthyridines having the general formula

    IN WHICH R1 and R2, which may be the same or different, are selected from H, OH and OCH3, and R3 is selected from H, Cl, Br and -COCO2C2H5.

    Abstract translation: 本发明涉及作为有用的治疗剂的新的吲哚衍生物。

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