Process for the production of
[1,1-dithienyl-(3)-1-hydroxypropyl-(3)]-[1-phenyl-1-hydroxypropyl-(2)]-a
mine and [1,1-dithienyl-(3)-propen-(1)-yl-(3)]-[1-phenylpropyl-(2)]-amine
    1.
    发明授权
    Process for the production of [1,1-dithienyl-(3)-1-hydroxypropyl-(3)]-[1-phenyl-1-hydroxypropyl-(2)]-a mine and [1,1-dithienyl-(3)-propen-(1)-yl-(3)]-[1-phenylpropyl-(2)]-amine 失效
    制备[1,1-二噻吩基 - (3)-1-羟基丙基 - (3)] - [1-苯基-1-羟丙基 - (2)] - 胺和[1,1-二噻吩基 - (3 ) - 丙烯 - (1) - 基 - (3)] - [1-苯基丙基 - (2)] - 胺

    公开(公告)号:US4175088A

    公开(公告)日:1979-11-20

    申请号:US867294

    申请日:1978-01-05

    CPC分类号: C07D333/16 C07D333/20

    摘要: [1,1-dithien-(3)-yl-1-hydroxy-(3)-propyl]-[1-phenyl-1-hydroxy-(2)-propyl]-amine is prepared by condensing thien-(3)-yl lithium with a .beta.-halogen propionic acid alkyl ester of the formula ##STR1## where R is a lower alkyl group and Hal is chlorine, bromine or iodine, in an inert medium at a temperature below -50.degree. C. to form a compound of the formula ##STR2## which is then reacted with 2-amino-1-hydroxy-1-phenylpropane in an inert medium in the presence of a basic compound. The product cn be converted to [1,1-dithien-(3)-yl-(1)-propen-(3)-yl]-[1-phenyl-(2)-propyl]-amine by dehydration.

    摘要翻译: 通过将噻吩(3) - (3) - (1) - 羟基 - (3) - 丙基] - [1-苯基-1-羟基 - (2) ) - 基锂与式(II)的β-卤代丙酸烷基酯反应,其中R是低级烷基,Hal是氯,溴或碘,在惰性介质中,温度低于-50℃ 形成式(III)的化合物,然后在碱性化合物的存在下,在惰性介质中与2-氨基-1-羟基-1-苯基丙烷反应。 通过脱水将产物转化为[1,1-二噻吩 - (3) - 基 - (1) - 丙烯 - (3) - 基] - [1-苯基 - (2) - 丙基] - 胺。

    Method of making thieno-pyridine derivatives
    3.
    发明授权
    Method of making thieno-pyridine derivatives 失效
    制备噻吩并吡啶衍生物的方法

    公开(公告)号:US06043368A

    公开(公告)日:2000-03-28

    申请号:US707658

    申请日:1996-09-04

    IPC分类号: C07D495/04 C07D333/14

    CPC分类号: C07D495/04

    摘要: The present invention provides a method of preparing thieno[3,2-c]pyridine derivatives of formula I: ##STR1## wherein R.sub.1 is selected from the group consisting of lower alkyl; lower alkylene phenyl; substituted lower alkylene phenyl wherein the phenyl is substituted from 1 to 3 times with lower alkyl, lower alkoxy, lower acyloxy, hydroxy, nitro and halo; lower alkylene naphthyl, lower alkylene thienyl; lower alkylene diphenyl; lower alkylene-hydroxy-phenyl; substituted lower alkylene-hydroxy-phenyl wherein the phenyl is substituted from 1 to 3 times with lower alkyl, lower alkoxy, lower acyloxy, hydroxy, nitro, and halo; lower alkylene-hydroxy-naphthyl; lower alkylene-hydroxy-thienyl; lower alkylene-hydroxy-diphenyl, and R.sub.2 is H or lower alkylene. The method comprises reacting a compound of a formula II: ##STR2## with a cyclic dioxy or cyclic dithio in the presence of catalyst.

    摘要翻译: 本发明提供制备式I的噻吩并[3,2-c]吡啶衍生物的方法:其中R 1选自低级烷基; 低级亚烷基苯基; 取代的低级亚烷基苯基,其中苯基与低级烷基,低级烷氧基,低级酰氧基,羟基,硝基和卤素取代1至3倍; 低级亚烷基萘基,低级亚烷基噻吩基; 低级亚烷基二苯基; 低级亚烷基 - 羟基苯基; 取代的低级亚烷基 - 羟基 - 苯基,其中苯基与低级烷基,低级烷氧基,低级酰氧基,羟基,硝基和卤素取代1〜3倍。 低级亚烷基 - 羟基 - 萘基; 低级亚烷基 - 羟基 - 噻吩基; 低级亚烷基 - 羟基 - 二苯基,R 2为H或低级亚烷基。 该方法包括在催化剂存在下使式II化合物与环状二氧基或环状二硫基反应。

    Fungicidal alpha-substituted acrylates
    5.
    发明授权
    Fungicidal alpha-substituted acrylates 失效
    杀真菌α-取代丙烯酸酯

    公开(公告)号:US4802913A

    公开(公告)日:1989-02-07

    申请号:US893272

    申请日:1986-08-05

    摘要: Compounds of formula (I): ##STR1## and stereoisomers thereof, wherein V is an oxygen or a sulphur atom; X and Y, which may be the same or different, are hydrogen or halogen atoms, or optionally substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted alkynyl, haloalkyl, alkoxy, haloalkoxy, optionally substituted aryloxy, optionally substituted arylalkoxy, optionally substituted acyloxy, optionally substituted amino, acylamino, nitro, nitrile, --CO.sub.2 R.sup.3, --CONR.sup.4 R.sup.5, or --COR.sup.6 groups; or the groups X and Y, when they are in adjacent positions on the phenyl ring, may join to form a fused ring, either aromatic or aliphatic, optionally containing one or more heteroatoms; and Z is optionally substituted methylene, optionally substituted amino, oxygen or sulphur and when Z is a substituted methylene group, the substituent may join the 2-position of the phenyl ring to form a non-aromatic fused ring; R.sup.1 and R.sup.2 are alkyl groups containing from one to four carbon atoms, optionally substituted with one or more halogen atoms; and R.sup.3, R.sup.4, R.sup.5 and R.sup.6, which may be the same or different, are hydrogen atoms or optionally substituted alkyl, cycloalkyl, alkenyl, alkynyl, optionally substituted aryl, optionally substituted aralkyl, or cycloalkylalkyl groups; and metal complexes thereof.

    摘要翻译: 式(I)化合物:其中V是氧或硫原子; X和Y可以相同或不同,是氢或卤素原子,或任选取代的烷基,任选取代的烯基,任选取代的芳基,任选取代的杂芳基,任选取代的炔基,卤代烷基,烷氧基,卤代烷氧基,任选取代的芳氧基, 取代的芳基烷氧基,任选取代的酰氧基,任选取代的氨基,酰氨基,硝基,腈,-CO 2 R 3,-CONR 4 R 5或-COR 6基团; 或基团X和Y当它们在苯环上的相邻位置时,可以连接形成任选含有一个或多个杂原子的芳族或脂族稠合的稠环; Z是任选取代的亚甲基,任选取代的氨基,氧或硫,当Z是取代的亚甲基时,取代基可以连接苯环的2-位,形成非芳香稠环; R1和R2是含有1-4个碳原子的烷基,任选地被一个或多个卤素原子取代; 可以相同或不同的R 3,R 4,R 5和R 6是氢原子或任选取代的烷基,环烷基,烯基,炔基,任选取代的芳基,任选取代的芳烷基或环烷基烷基; 及其金属络合物。

    Amine derivatives
    6.
    发明授权
    Amine derivatives 失效
    胺衍生物

    公开(公告)号:US4317819A

    公开(公告)日:1982-03-02

    申请号:US213680

    申请日:1980-12-05

    摘要: The invention provides compounds of general formula ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in whichY and Z, which may be the same or different, each represent oxygen, sulphur, .dbd.CHNO.sub.2 or .dbd.NR.sub.3 where R.sub.3 is hydrogen, nitro, cyano, lower alkyl, aryl, alkylsulphonyl or arylsulphonyl;p has a value from 2 to 12;R.sub.1 represents ##STR2## in which R.sub.4 and R.sub.5 which may be the same or different, each represent hydrogen, lower alkyl, cycloalkyl, lower alkenyl, aralkyl or lower alkyl interrupted by an oxygen atom or a group >N-R.sub.6 in which R.sub.6 represents hydrogen or lower alkyl, or R.sub.4 and R.sub.5 together with the nitrogen atom to which they are attached form a 5 to 7-membered saturated heterocyclic ring which may contain an additional oxygen atom or the group >NR.sub.6 ;Q represents a furan or thiophen ring in which incorporation into the rest of the molecule is through bonds at the 2 and 5 positions, or a benzene ring in which incorporation into the rest of the molecule is through bonds at the 1 and 3 or 1 and 4 positions;X represents --CH.sub.2 --, --O-- or --S--;n represents zero or 1;m represents 2, 3 or 4 and Alk represents a straight chain alkylene group of 1 to 3 carbon atoms,andR.sub.2 represents lower alkyl or the group--(CH.sub.2).sub.y E(CH.sub.2).sub.x Gin whichy represents 2, 3 or 4 or can additionally represent zero or 1 when E is a --CH.sub.2 -- group, x represents zero, 1 or 2;E represents --CH.sub.2 --, --O-- or --S--; andG represents a monocyclic 5 or 6 membered carbocyclic or heterocyclic aromatic ring, or G represents the group ##STR3## where Q' represents any of the rings defined for Q; Alk' represents any of the groups defined for Alk; and R.sub.4 ' and R.sub.5 ' which may be the same or different represent any of the groups defined for R.sub.4 or R.sub.5.The compounds of formula (I) have pharmacological activity as selective histamine H.sub.2 -antagonists.

    摘要翻译: 本发明提供了通式(I)的化合物及其生理上可接受的盐,水合物和生物前体,其中Y和Z可以相同或不同,各自表示氧,硫,= CHNO 2或= NR 3,其中R 3 是氢,硝基,氰基,低级烷基,芳基,烷基磺酰基或芳基磺酰基; p的值为2到12; R 1表示其中可以相同或不同的R 4和R 5各自表示氢,低级烷基,环烷基,低级烯基,芳烷基或被氧原子间隔的低级烷基或基团> N-R6,其中R 6表示 氢或低级烷基,或R4和R5与它们所连接的氮原子一起形成可含有另外的氧原子或基团> NR 6的5至7元饱和杂环; Q表示呋喃或噻吩环,其中与分子的其余部分结合通过2和5位的键,或苯环,其中结合到分子的其余部分通过1和3或1的键和 4个职位; X表示-CH 2 - , - O-或-S-; n表示0或1; m表示2,3或4,Alk表示1〜3个碳原子的直链亚烷基,R2表示低级烷基或 - (CH2)yE(CH2)xG,y表示2,3或4或可以 当E是-CH 2 - 基时,x代表0或1; E表示-CH 2 - , - O-或-S-; 并且G表示单环5或6元碳环或杂环芳环,或G表示基团,其中Q'表示为Q定义的任何环; Alk'代表为Alk定义的任何组; 和可以相同或不同的R 4'和R 5'表示对于R 4或R 5定义的任何基团。 式(I)化合物具有作为选择性组胺H2拮抗剂的药理学活性。

    Amine derivatives
    7.
    发明授权
    Amine derivatives 失效
    胺衍生物

    公开(公告)号:US4264614A

    公开(公告)日:1981-04-28

    申请号:US95065

    申请日:1979-11-16

    摘要: The invention provides compounds of general formula ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in whichY and Z, which may be the same or different, each represent oxygen, sulphur, =CHNO.sub.2 or =NR.sub.3 where R.sub.3 is hydrogen, nitro, cyano, lower alkyl, aryl, alkylsulphonyl or arylsulphonyl;p has a value from 2 to 12;R.sub.1 represents ##STR2## in which R.sub.4 and R.sub.5 which may be the same or different, each represent hydrogen, lower alkyl, cycloalkyl, lower alkenyl, aralkyl or lower alkyl interrupted by an oxygen atom or a group >N-R.sub.6 in which R.sub.6 represents hydrogen or lower alkyl, or R.sub.4 and R.sub.5 together with the nitrogen atom to which they are attached form a 5 to 7-membered saturated heterocyclic ring which may contain an additional oxygen atom or the group >NR.sub.6 ;Q represents a furan or thiophen ring in which incorporation into the rest of the molecule is through bonds at the 2 and 5 positions, or a benzene ring in which incorporation into the rest of the molecule is through bonds at the 1 and 3 or 1 and 4 positions;X represents --CH.sub.2 --, --O-- or --S--;n represents zero or 1;m represents 2, 3 or 4 andAlk represents a straight chain alkylenegroup of 1 to 3 carbon atoms;and R.sub.2 represents lower alkyl or the group--(CH.sub.2).sub.y E(CH.sub.2).sub.x Gin whichY represents 2, 3 or 4 or can additionallyrepresent zero or 1 when E is a --CH.sub.2 -- group;x represents zero, 1 or 2;E represents --CH.sub.2 --, --0-- or --S--; andG represents a monocyclic 5 or 6 membered carbocyclic or heterocyclic aromatic ring, or G represents the group ##STR3## where Q' represents any of the rings defined for Q;Alk' represents any of the groups defined for Alk;and R.sub.4 ' and R.sub.5 ' which may be the same or different represent any of the groups defined for R.sub.4 or R.sub.5.The compounds of formula (I) have pharmacological activity as selective histamine H.sub.2 -antagonists.

    摘要翻译: 本发明提供了通式(I)的化合物及其生理上可接受的盐,水合物和生物前体,其中Y和Z可以相同或不同,各自表示氧,硫,= CHNO 2或= NR 3,其中R 3 是氢,硝基,氰基,低级烷基,芳基,烷基磺酰基或芳基磺酰基; p的值为2到12; R 1表示其中可以相同或不同的R 4和R 5各自表示氢,低级烷基,环烷基,低级烯基,芳烷基或被氧原子间隔的低级烷基或基团> N-R6,其中R 6表示 氢或低级烷基,或R4和R5与它们所连接的氮原子一起形成可含有另外的氧原子或基团> NR 6的5至7元饱和杂环; Q表示呋喃或噻吩环,其中与分子的其余部分结合通过2和5位的键,或苯环,其中结合到分子的其余部分通过1和3或1的键和 4个职位; X表示-CH 2 - , - O-或-S-; n表示0或1; m表示2,3或4,Alk表示1〜3个碳原子的直链亚烷基; 并且R 2表示低级烷基或基团 - (CH 2)y E(CH 2)x G,其中Y表示2,3或4,或者当E是-CH 2 - 基时,可以另外表示0或1; x表示零,1或2; E表示-CH 2 - , - O-或-S-; 并且G表示单环5或6元碳环或杂环芳环,或G表示基团,其中Q'表示为Q定义的任何环; Alk'代表为Alk定义的任何组; 和可以相同或不同的R 4'和R 5'表示对于R 4或R 5定义的任何基团。 式(I)化合物具有作为选择性组胺H2拮抗剂的药理学活性。

    Sulfoxyalkylthiophene and Process for Producing the Same
    8.
    发明申请
    Sulfoxyalkylthiophene and Process for Producing the Same 有权
    磺酰烷基噻吩及其制备方法

    公开(公告)号:US20070260071A1

    公开(公告)日:2007-11-08

    申请号:US10580864

    申请日:2004-11-17

    申请人: Hideo Suzuki

    发明人: Hideo Suzuki

    IPC分类号: C07D333/14

    CPC分类号: C07D333/16

    摘要: A sulfoalkylthiophene compound of the following formula [1] and a hydroxyalkylthiophene compound of the following formula [2], from which a useful π-conjugated conductive polymer monomer capable of oxidation polymerization can be provided: (wherein R is a hydrogen atom, an alkali metal atom or an alkaline earth metal atom, and n is an integer of 1 to 3) (wherein n is as defined above).

    摘要翻译: 下式[1]的磺基烷基噻吩化合物和下式[2]的羟基烷基噻吩化合物可以由其提供能够进行氧化聚合的有用的π共轭导电性高分子单体:(式中,R为氢原子,碱 金属原子或碱土金属原子,n为1〜3的整数)(n为上述定义)。