Novel 1-alkyl-1-arenesulfonyl-2-alkoxycarbonylsulfenylhydrazines having
antineoplastic activity
    2.
    发明授权
    Novel 1-alkyl-1-arenesulfonyl-2-alkoxycarbonylsulfenylhydrazines having antineoplastic activity 失效
    具有抗肿瘤活性的新型1-烷基-1-芳烃磺酰基-2-烷氧基羰基亚磺酰肼

    公开(公告)号:US4849563A

    公开(公告)日:1989-07-18

    申请号:US142354

    申请日:1987-12-28

    IPC分类号: C07C329/02

    CPC分类号: C07C329/02

    摘要: Compounds of the formula: ##STR1## wherein R.sub.1 s an alkyl of 1-6 carbon atoms, benzyl, phenyl, or phenyl substituted by halogen, alkoxy of 1 to 4 carbon atoms, alkyl of 1 to 4 carbon atoms, amino, or carbonyl substituents, or --RN(R').sub.2 wherein R and R' are each independently an alkyl of 1 to 4 carbon atoms; R.sub.2 is an aromatic substituent selected from the group consisting of phenyl, benzyl, and naphthyl, and A is an aromatic substitution selected from the group consisting of hydrogen, alkyl of 1-4 carbon atoms, alkoxy of 1-4 carbon atoms, halogen, --NO.sub.2, --NH.sub.2, --COOH, and --NHCOCH.sub.3. The compounds have been found to be alkylating agents having antineoplastic activity for use in inhibiting the growth of tumors.

    摘要翻译: 下式的化合物:其中R 1为1-6个碳原子的烷基,苄基,苯基或被卤素取代的苯基,1至4个碳原子的烷氧基,1至4个碳原子的烷基,氨基或羰基 取代基或-RN(R')2,其中R和R'各自独立地为1至4个碳原子的烷基; R2是选自苯基,苄基和萘基的芳香族取代基,A是选自氢,1-4个碳原子的烷基,1-4个碳原子的烷氧基,卤素, -NO 2,-NH 2,-COOH和-NHCOCH 3。 已经发现这些化合物是具有抗肿瘤活性的烷基化剂,用于抑制肿瘤的生长。

    Process for the production of alkyl thiochloroformates
    3.
    发明授权
    Process for the production of alkyl thiochloroformates 失效
    用于生产烷基硫代氯甲酸酯的方法

    公开(公告)号:US4820856A

    公开(公告)日:1989-04-11

    申请号:US108996

    申请日:1987-10-16

    CPC分类号: C07C329/00

    摘要: The subject of the invention is a new process for the preparation of alkyl thiochloroformates.The process according to the invention consists in reacting phosgene with a mercaptan in the presence of a catalyst which is a hexaalkylguanidinium chloride or the corresponding hydrochloride of general formula: ##STR1## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 represent alkyl radicals containing 1 to 4 carbon atoms and in which n may take either the value 0 or the value 1.The preferred catalysts are hexamethylguanidinium chloride and its hydrochloride.The process according to the invention enables very pure alkyl thiochloroformates to be obtained with milder operating conditions and simplified purification operations.

    摘要翻译: 本发明的主题是制备烷基硫代氯甲酸酯的新方法。 根据本发明的方法在于使光气与硫醇在催化剂存在下反应,催化剂是六烷基氯化胍或通式为:其中R 1,R 2,R 3,R 4,R 5和R 6表示烷基的相应盐酸盐 含有1至4个碳原子的基团,其中n可以取0或值1.优选的催化剂是六甲基胍氯化物及其盐酸盐。 根据本发明的方法使得能够在更温和的操作条件和简化的纯化操作中获得非常纯的烷基硫代氯甲酸酯。

    Fluorinated thiocarbonic acid ester-fluorides
    4.
    发明授权
    Fluorinated thiocarbonic acid ester-fluorides 失效
    氟化硫代碳酸酯 - 氟化物

    公开(公告)号:US4564478A

    公开(公告)日:1986-01-14

    申请号:US670693

    申请日:1984-11-13

    CPC分类号: C07C329/00 C07C323/00

    摘要: Novel fluorinated thiocarbonic acid ester-fluorides of the formula ##STR1## in which R.sup.1 represents alkyl, cycloalkyl or optionally substituted aryl andR.sup.2 and R.sup.3 independently of one another represent hydrogen or alkyl, orR.sup.1 and R.sup.2 together represent an alkylene chain,a new process for the preparation of the new compounds and their use as intermediates for the preparation of compounds having herbicidal properties.Novel intermediates of the formulae ##STR2## in which R.sup.2 and R.sup.3 have the above-mentioned meaning,R.sup.4 is optionally substituted aryl,R.sup.5 is alkyl or cycloalkyl, andX is fluorine or chlorine, at least one X representing chlorine.

    摘要翻译: 式(I)的新型氟代硫代碳酸酯 - 氟化物,其中R 1表示烷基,环烷基或任选取代的芳基,R 2和R 3彼此独立地表示氢或烷基,或者R 1和R 2一起表示亚烷基链, 用于制备新化合物的新方法及其作为制备具有除草性的化合物的中间体的用途。 其中R 2和R 3具有上述含义的式“IMAGE”的新型中间体,R 4是任选取代的芳基,R 5是烷基或环烷基,X是氟或氯,至少一个X代表氯。

    Process for the preparation of pyrazole carboxylic acid amides
    5.
    发明授权
    Process for the preparation of pyrazole carboxylic acid amides 有权
    制备吡唑羧酸酰胺的方法

    公开(公告)号:US08895757B2

    公开(公告)日:2014-11-25

    申请号:US13981913

    申请日:2012-01-25

    摘要: The invention relates to a process for the preparation of 3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxylic acid (9-dichloromethylene-1,2,3,4-tetrahydro-1,4-methano-naphthalen-5-yl)-amide by acylating the oxime oxygen of the compound of formula (VIII), in the presence of a solvent and an acylating agent of formula (XI) R1C(X)—CI (XI); wherein X is oxygen or sulfur; R1 is chloro if X is oxygen or sulfur; or R1 is C1-C6alkoxy, CH3—C(═CH2)—O—, phenoxy or trichloromethoxy if X is oxygen; and a) if R1 is chloro and the compound of formula (XI) was added to the compound of formula (VIII); reacting the so obtained product of formula (XIIa) wherein X is oxygen or sulfur; with the compound of formula (IX) b) if R1 is chloro and the compound of formula (VIII) was added to the compound of formula (XI); or R1 is C1-C6alkoxy, CH3—C(═CH2)—O—, phenoxy or trichloromethoxy if X is oxygen; reacting the so obtained product of formula (XII) wherein X is oxygen or sulfur; R1 is chloro if X is oxygen or sulfur; or R1 is C1-C6alkoxy, CH3—C(═CH2)—O—, phenoxy or trichloromethoxy if X is oxygen; with the compound of formula (IX).

    摘要翻译: 本发明涉及制备3-二氟甲基-1-甲基-1H-吡唑-4-羧酸(9-二氯亚甲基-1,2,3,4-四氢-1,4-亚甲基 - 萘-5 (XI)R1C(X)-CⅠ(XI)的溶剂和酰化剂的存在下酰化式(Ⅷ)化合物的肟氧; 其中X是氧或硫; 如果X是氧或硫,则R1是氯; 或者如果X是氧,则R1是C1-C6烷氧基,CH3-C(= CH2)-O-,苯氧基或三氯甲氧基; 和a)如果R1是氯,并且将式(XI)化合物加入到式(VIII)化合物中; 使所得的式(XIIa)化合物与X为氧或硫反应; 与式(Ⅸ)化合物b)如果R 1是氯,并将式(Ⅷ)化合物加到式(Ⅺ)化合物中; 或者如果X是氧,则R1是C1-C6烷氧基,CH3-C(= CH2)-O-,苯氧基或三氯甲氧基; 使所得的式(XII)化合物(其中X是氧或硫)反应; 如果X是氧或硫,则R1是氯; 或者如果X是氧,则R1是C1-C6烷氧基,CH3-C(= CH2)-O-,苯氧基或三氯甲氧基; 与式(IX)的化合物反应。

    Process for the preparation of thiochloroformates
    9.
    发明授权
    Process for the preparation of thiochloroformates 失效
    制备硫代氯甲酸酯的方法

    公开(公告)号:US4340746A

    公开(公告)日:1982-07-20

    申请号:US181428

    申请日:1980-08-26

    CPC分类号: C07C329/00

    摘要: Thiochloroformates are prepared by reaction of mercaptans with phosgene in the presence of carboxylic acid amides and/or urea derivatives as catalysts in amounts smaller than hitherto known for this application. The amounts range from about 0.02 to 0.2 mol %, relative to the corresponding starting mercaptan. Despite the small amounts of catalyst the reaction proceeds as with the use of larger catalyst amounts; however, work-up is simplified and the product yields are increased in most cases.

    摘要翻译: 在羧酸酰胺和/或脲衍生物作为催化剂的存在下,硫醇与光气反应制备硫代氯甲酸酯,其量小于迄今为止已知的用于本申请的量。 相对于相应的起始硫醇,其量为约0.02至0.2摩尔%。 尽管催化剂的量少,反应也随着使用较大的催化剂量而进行; 然而,在大多数情况下,后处理被简化,产品产量增加。