Method of preparing chroman derivatives, and synthesis intermediates
    3.
    发明授权
    Method of preparing chroman derivatives, and synthesis intermediates 失效
    制备色氨酸衍生物的方法和合成中间体

    公开(公告)号:US5071991A

    公开(公告)日:1991-12-10

    申请号:US456491

    申请日:1989-12-26

    CPC分类号: C07D213/64 C07D405/04

    摘要: The invention describes a method of synthesizing a compound of the formula ##STR1## in which X=O or NR,Z=an electron-attracting group,R=H, CN or NO.sub.2,R.sub.1 +R.sub.2 +N--C.dbd.X=a 5-membered or 6-membered heterocycle, andR.sub.3 =H, R.sub.4 =OH or R.sub.3 +R.sub.4 =a bond,said method involving intermediates of the formula ##STR2## in which R.sub.5 =H, Br or N(R.sub.1)CXR.sub.2. This method of synthesis does not involve the epoxide derivative of the chroman.The novel compounds of formula (IX) form a further subject of the invention.

    摘要翻译: 本发明描述了合成其中X = O或NR,Z =吸电子基团R = H,CN或NO 2的式(I)化合物的方法,R1 + R2 + NC = X = 5元或6元杂环,并且R 3 = H,R 4 = OH或R 3 + R 4 =一个键,所述方法涉及其中R 5 = H,Br或N(R 1) )CXR2。 这种合成方法不涉及苯并二氢吡喃的环氧化物衍生物。 式(IX)的新化合物形成本发明的另一个主题。

    Use of 2,2-dimethylchroman-3-ol derivatives in the treatment of asthma
    9.
    发明授权
    Use of 2,2-dimethylchroman-3-ol derivatives in the treatment of asthma 失效
    使用2,2-二甲基苯并二氢吡喃-3-醇衍生物治疗哮喘

    公开(公告)号:US5284838A

    公开(公告)日:1994-02-08

    申请号:US19314

    申请日:1993-02-18

    CPC分类号: C07D405/04 C07F9/65586

    摘要: The invention relates to 2,2-dimethylchroman-3-ol derivatives of the formula: ##STR1## in which: A, between N and CO, represents the group --CH.dbd.CH--E.dbd.CH-- or the group ##STR2## Z represents a halogen or a cyano, acetyl, trifluoroacetyl, nitro, alkylthio, carboxyl, phosphono, dial-koxyphosphoryl or alkoxycarbonyl group, the alkylthio and alkoxy groups containing from 1 to 3 carbon atoms;E represents a nitrogen atom or a group C(R.sub.4);R.sub.1 represents hydrogen, a methyl group or a hydroxyl group and R.sub.2 and R.sub.3 each independently represent hydrogen or a methyl group, it being possible for only one of the substituents R.sub.1, R.sub.2 and R.sub.3 to be methyl; andR.sub.4 represents a hydrogen atom, a halogen atom, a methyl group or a hydroxyl group;and to the pharmaceutically acceptable salts of the phosphono or carboxyl group.These derivatives have an antiarrhythmic, antiasthma and antihypertensive activity.

    摘要翻译: 本发明涉及下式的2,2-二甲基苯并二氢吡喃-3-醇衍生物:其中:A在N和CO之间代表基团-CH = CH-E = CH-或基团< Z表示卤素或氰基,乙酰基,三氟乙酰基,硝基,烷硫基,羧基,膦酰基,二烷氧基磷酰基或烷氧基羰基,含有1至3个碳原子的烷硫基和烷氧基; E表示氮原子或C(R4)基团; R1表示氢,甲基或羟基,R2和R3各自独立地表示氢或甲基,只有一个取代基R 1,R 2和R 3可以是甲基; R 4表示氢原子,卤素原子,甲基或羟基; 和膦酰基或羧基的药学上可接受的盐。 这些衍生物具有抗心律失常,抗哮喘和抗高血压作用。