Optically active chiral diphosphine ligands
    2.
    发明授权
    Optically active chiral diphosphine ligands 失效
    光学活性的手性二膦配体

    公开(公告)号:US06794525B2

    公开(公告)日:2004-09-21

    申请号:US10356233

    申请日:2003-01-31

    IPC分类号: C07F1500

    摘要: An (R) or (S) chiral diphosphine of formula (I): wherein R and R1, which can be identical or different, represent an optionally saturated C1-10 alkyl group, an optionally saturated C3-9 cycloalkyl group, a C5-10 aryl group, the groups being optionally substituted by a halogen, a hydroxy, a C1-5 alkoxy, an amino, a sulfino, a sulonfyl, with R4 representing an alkyl, an alkoxy or an alkylcarbonyl, the alkyl, cycloalkyl, aryl groups optionally including one or more heteroatoms, or R and R1 together represent an optionally saturated C2-6 substituted alkyl group, an optionally saturated C3-9 cycloalkyl group, a C5-10 aryl group, the cycloalkyl or aryl groups being optionally substituted by a C1-5 alkyl, a halogen, a hydroxy, a C1-5 alkoxy, an amino, a sulfino, a sulonfyl, with R4 representing an alkyl, an alkoxy or an alkylcarbonyl, the alkyl, cycloalkyl, aryl groups optionally including one or more heteroatoms, R2 and R3, which can be identical or different, represent an optionally saturated C3-8 cycloalkyl group, a C6-10 aryl group, the groups being optionally substituted by a halogen, a hydroxy, a C1-5 alkoxy, an amino, a sulfino, a sulonfyl, with R4 representing an alkyl, an alkoxy or an alkylcarbonyl, the cycloalkyl, aryl groups optionally including one or more heteroatoms, or R2 and R3 together form an optionally saturated C4-8 cyclic group, a C6-10 aryl group, the groups being optionally substituted by a halogen, a hydroxy, a C1-5 alkoxy, an amino, a sulfino, a sulonfyl, with R4 representing an alkyl, an alkoxy or an alkylcarbonyl, the cyclic and aryl groups optionally including one or more heteroatoms.

    摘要翻译: 式(I)的(R)或(S)手性二膦:其中R和R 1可以相同或不同,表示任选饱和的C 1-10烷基,任选饱和的C 3-9环烷基, 10芳基,该基团任选被卤素,羟基,C 1-5烷氧基,氨基,亚磺酰基,磺酰基取代,R 4表示烷基,烷氧基或烷基羰基,烷基,环烷基,芳基 任选地包括一个或多个杂原子,或R和R 1一起表示任选饱和的C 2-6取代烷基,任选饱和的C 3-9环烷基,C 5-10芳基,环烷基或芳基任选被C 1 -5-烷基,卤素,羟基,C 1-5烷氧基,氨基,亚磺酰基,磺酰基,其中R 4表示烷基,烷氧基或烷基羰基,烷基,环烷基,芳基,任选地包括一个或多个杂原子 可以相同或不同的R 2和R 3表示任选饱和的 C 3〜C 8环烷基,C 6-10芳基,所述基团任选被卤素,羟基,C 1-5烷氧基,氨基,亚磺酰基,磺酰基取代,R 4表示烷基,烷氧基或 烷基羰基,环烷基,任选地包括一个或多个杂原子的芳基,或者R 2和R 3一起形成任选饱和的C 4-8环基,C 6-10芳基,该基团任选被卤素取代,羟基, C 1-5烷氧基,氨基,亚磺酰基,磺酰基,其中R 4表示烷基,烷氧基或烷基羰基,环和芳基任选地包括一个或多个杂原子。

    Process for the preparation of
(+/-)3-(3,4-dichlorophenyl)-2-dimethylamino-2-methylpropan-1-OL or
cericlamine (INN)
    4.
    发明授权
    Process for the preparation of (+/-)3-(3,4-dichlorophenyl)-2-dimethylamino-2-methylpropan-1-OL or cericlamine (INN) 失效
    制备(+/-)3-(3,4-二氯苯基)-2-二甲基氨基-2-甲基丙-1-醇或十六烷胺(INN)的方法

    公开(公告)号:US6121491A

    公开(公告)日:2000-09-19

    申请号:US381118

    申请日:1999-12-20

    摘要: Process for the preparation of cericlamine which consists: i) in arylating methacrylic acid with the diazonium chloride of 3,4-dichloroaniline, to obtain (+/-)2-chloro-3-(3,4-dichlorophenyl)-2-methylpropionic acid, ii) in aminating the acid with dimethylamine, to obtain (+/-)3-(3,4-dichlorophenyl)-2-dimethylamino-2-methylpropionic acid, or an alkaline metal salt thereof, iii) in esterifying the amino-acid or its salt, then, iv) in reducing the ester by a metal or organometal hydride to obtain (+/-)3-(3,4-dichlorophenyl)-2-dimethylamino-2-methyl-propan-1-ol.

    摘要翻译: PCT No.PCT / EP98 / 02213 371 1999年12月20日第 102(e)日期1999年12月20日PCT提交1998年4月6日PCT公布。 公开号WO98 / 45248 日期1998年10月15日制备铈胺的方法,其包括:i)在甲基丙烯酸中与3,4-二氯苯胺的重氮氯化物进行芳基化,得到(+/-)2-氯-3-(3,4-二氯苯基 )-2-甲基丙酸,ii)用二甲胺胺化酸,得到(+/-)3-(3,4-二氯苯基)-2-二甲基氨基-2-甲基丙酸或其碱金属盐,iii )中,然后iv)在金属或有机金属氢化物还原酯时,得到(+/-)3-(3,4-二氯苯基)-2-二甲基氨基-2-甲基 - 丙-1-醇