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    • 65. 发明授权
    • Process for preparation of glycidyl ether
    • 缩水甘油醚的制备方法
    • US5359097A
    • 1994-10-25
    • US571543
    • 1990-08-22
    • Kiyoshi KawamuraTomio Ota
    • Kiyoshi KawamuraTomio Ota
    • C07D301/28C07D303/22C07D405/12C07D407/12C07D417/12C07D311/04
    • C07D303/22C07D407/12
    • A process is provided for preparation of a glycidyl ether represented by the general formula ##STR1## wherein A represents an aryl group optionally having a substituent or a heteroaryl group optionally having a substituent, and the carbon atom marked with * is an asymmetric carbon,which comprises reacting an aryl alcohol represented by the general formulaA--OH (I)wherein A is as defined above,with an epihalohydrin in the presence of a quaternary ammonium salt; and, if necessary, further treating the reaction product with a base. According to the present process, it is possible to prepare by simple procedures and in a high optical purity glycidyl ethers of the above formula (II) useful as an intermediate for preparation of medicines, particularly medicines having .beta.-adrenoreceptor blocking action or the like.
    • PCT No.PCT / JP89 / 01293 Sec。 371 1990年7月18日第 102(e)日期1990年7月18日PCT提交1989年12月25日PCT公布。 出版物WO90 / 07506 日本1990年7月12日提供了一种制备由任选具有取代基的通式或由任选具有取代基的杂芳基表示的缩水甘油醚的方法,标有*的碳原子是不对称碳,其包括使 由季铵盐存在下的表卤代醇,由通式A-OH(I)表示的芳基醇,其中A如上所定义; 并且如果需要,用碱进一步处理反应产物。 根据本方法,可以通过简单的方法和上述式(II)的高光学纯度的缩水甘油醚制备,其可用作制备药物的中间体,特别是具有β-肾上腺素受体阻断作用的药物等。
    • 69. 发明授权
    • Methylmethioninesulfonium compounds, process for their preparation, and
pharmaceutical compositions containing them
    • 甲基亚氨基锍化合物,其制备方法和含有它们的药物组合物
    • US4216225A
    • 1980-08-05
    • US906567
    • 1978-05-16
    • Masami ShiratsuchiKiyoshi KawamuraHisashi KuniedaNaoki MachidaToshihiro AkashiMasahiko Nagakura
    • Masami ShiratsuchiKiyoshi KawamuraHisashi KuniedaNaoki MachidaToshihiro AkashiMasahiko Nagakura
    • A61K31/195A61K31/16A61K31/22A61P1/04C07C67/00C07C325/00C07C381/12C07D213/82A61K31/55A61K31/215
    • C07D213/82
    • Methylmethioninesulfonium compounds of the formula ##STR1## wherein X.crclbar. represents an anion;R.sup.1 represents a hydrogen atom or an acyl group of the formula -COR.sup.3 in which R.sup.3 represents an alkyl group with 1 to 20 carbon atoms, the group --CH.sub.2).sub.2 COOH or the group ##STR2## in which Z represents a direct bond or a methylene or vinylene linkage, Y represents C or N, R.sup.4 represents a member selected from the class consisting of a hydrogen atom, lower alkyl groups, lower alkoxy groups, di-lower-alkylamino groups and a sulfamoyl group, n is a number of 1 to 3, and two or more R.sup.4 groups may be identical or different; andR.sup.2 represents the group --COOR.sup.5 in which R.sup.5 represents a hydrogen atom, an alkyl group with 1 to 5 carbon atoms or a metal- or metal complex-forming moiety, or the group ##STR3## in which R.sup.6 groups may be identical or different, and each represent a hydrogen atom or an alkyl group with 1 to 5 carbon atoms, with the proviso that when R.sup.1 represents a hydrogen atom, R.sup.2 is not --COOH; when R.sup.1 represents a hydrogen atom and R.sup.2 represents --CONH.sub.2, X.crclbar. is not Cl.crclbar.; and when R.sup.1 is --COCH.sub.3 and R.sup.2 is --COOCH.sub.3, X.crclbar. is not I.crclbar..The compounds can be easily prepared from methionine as a starting material by a combination of known unit reactions such as methylsulfonium-forming reaction, acylation, amidation, esterification and metal salt-forming reaction. These compounds are especially useful for treating ulcers.
    • 其中X( - )表示阴离子的式“IMAGE”的甲基甲硫氨onium化合物; R 1表示氢原子或式-COR 3的酰基,其中R 3表示具有1至20个碳原子的烷基,基团-CH 2)2 COOH或其中Z表示直接键或基团 亚甲基或亚乙烯基,Y表示C或N,R4表示选自氢原子,低级烷基,低级烷氧基,二低级烷基氨基和氨磺酰基的成员,n为1 至3个,并且两个或更多个R 4基团可以相同或不同; 并且R 2表示其中R 5表示氢原子,具有1至5个碳原子的烷基或金属或金属络合物形成部分的基团-COOR 5或其中R6基团可以相同或不同的基团 并且各自表示氢原子或具有1至5个碳原子的烷基,条件是当R 1表示氢原子时,R 2不是-COOH; 当R 1表示氢原子且R 2表示-CONH 2时,X( - )不是Cl( - ); 当R1是-COCH3且R2是-COOCH3时,X( - )不是I( - )。 通过已知的单元反应如甲基锍形成反应,酰化,酰胺化,酯化和金属盐形成反应的组合,可以容易地从甲硫氨酸作为原料制备化合物。 这些化合物特别适用于治疗溃疡。