Aliphatic thioethers
    2.
    发明授权
    Aliphatic thioethers 失效
    脂族硫醚

    公开(公告)号:US4649215A

    公开(公告)日:1987-03-10

    申请号:US748656

    申请日:1985-06-25

    摘要: Novel asymmetric thioethers of the formula ##STR1## in which R.sup.1 represents a C.sub.1-3 -alkyl radical or a C.sub.1-3 -hydroxyalkyl radical of which the hydroxy group may be in esterified form,R.sup.2 represents an optionally unsaturated aliphatic radical having from 5 to 15 carbon atoms,R.sup.3 represents hydroxy, alkoxy or an optionally substituted amino group, and-X- represents a single bond, a methylene group or an optionally N-acylated primary aminomethylene groupwherein the O-atom of the hydroxy group is in the transconfiguration relative to the S-atom, are effective as leucotriene-antagonists since they eliminate the contractions of smooth muscles caused by leucotrienes and are therefore suitable for the treatment of allergic, especially asthmatic, conditions.

    摘要翻译: 式(I)的新型不对称硫醚,其中R 1表示C 1-3 - 烷基或羟基可以被酯化形成的C 1-3 - 羟基烷基,R 2表示具有 5至15个碳原子,R 3表示羟基,烷氧基或任选取代的氨基,-X-表示单键,亚甲基或任选N-酰化的伯氨基亚甲基,其中羟基的O-原子是 在相对于S原子的反式构型中,作为白三烯拮抗剂是有效的,因为它们消除了由白三烯引起的平滑肌的收缩,因此适用于治疗变态反应,特别是哮喘病症。

    Method of sulfation
    3.
    发明授权
    Method of sulfation 失效
    硫酸化方法

    公开(公告)号:US4444682A

    公开(公告)日:1984-04-24

    申请号:US439312

    申请日:1982-11-04

    摘要: A method for sulfating a hydroxy amino acid or a residue of such an amino acid in a peptide by reaction with a reagent which is a tertiaryammonium salt of acetylsulfuric acid having the formula:[CH.sub.3 COOSO.sub.3 ].sup.- [R].sup.+wherein R is triethylamine, ethyldiisopropylamine, pyridine, 4-methylmorpholine or 4-N,N-dimethylaminopyridine. The .alpha.-amino group and any other labile side chains present may be protected or may be left unprotected at the time the sulfation takes place.

    摘要翻译: 通过与具有下式的[CH3COOSO3] - [R] +的乙酰硫酸的叔铵盐的试剂反应来硫酸化肽中的羟基氨基酸或这种氨基酸的残基的方法,其中R是三乙胺,乙基二异丙胺 ,吡啶,4-甲基吗啉或4-N,N-二甲基氨基吡啶。 存在的α-氨基和任何其它不稳定的侧链可以被保护,或者可能在硫酸化发生时不被保护。

    Process for producing sulfones
    6.
    发明授权
    Process for producing sulfones 失效
    生产砜的方法

    公开(公告)号:US3980535A

    公开(公告)日:1976-09-14

    申请号:US474167

    申请日:1974-05-29

    CPC分类号: C07D333/72 C25B3/00

    摘要: Sulfones are produced by reacting an organic compound R--X (where X is a substituent on the organic radical R replaceable by SO.sub.2.sup.- ion) in an aprotic organic medium which may be the compound itself, with SO.sub.2.sup.- ions produced by electrolysis upon introduction of sulfur dioxide into the system. Any of a wide range of sulfones or polysulfones having surfactant and fabric-treating (finishing) or therapeutic properties or serving as materials for the manufacture of plastics may be made in this manner.

    摘要翻译: 砜是通过有机化合物RX(其中X是可由SO 2 - 离子可以被有机基团R取代的取代基)在可以是化合物本身的非质子有机介质中与通过电解产生的SO 2 - 将二氧化硫引入系统。 任何具有表面活性剂和织物处理(整理)或治疗性质的或用作塑料制造材料的砜或聚砜的方法可以以这种方式进行。