CAS: 2430-27-5; 2-Propylpentanamide

上下游产品

2-cyano-2-propyl-valeric acid ethanol 2,2-dipropylmalononitrile valproyl chloride di-N-propyl acetonitrile valproic acid N-phenethyl-2-propylpentanamide benzyl 2-propylpentanoate

2,2-二-正丙基乙酰基氯置于ammonium Hydroxide体系中,用 水,乙腈 用作溶剂,化学反应 2.0H,反应生成丙戊酰胺
参考文献:丙戊酸类似物的新型酰胺和尿素衍生物的合成及抗痛觉过敏和抗惊厥活性的评价
标题:丙戊酸类似物的新型酰胺和尿素衍生物的合成及抗痛觉过敏和抗惊厥活性的评价
摘要:丙戊酸(vpa,1)是主要的广谱抗癫痫药和中枢神经系统药物,广泛用于治疗癫痫,双相情感障碍和偏头痛.Vpa的临床使用受到两种严重且危及生命的副作用,致畸性和肝毒性的限制.合成了许多vpa类似物及其酰胺,N-甲基酰胺和尿素衍生物,并在神经性疼痛和癫痫的动物模型中进行了评估.其中,两种酰胺和两种尿素衍生物(1)作为抗神经痛药的效价最高,酰胺(19和20)的ed 50值分别为49和51 Mg / Kg,尿素衍生物的ed 50值为49和74 Mg / Kg. (29和33).19,20,和29是等效于加巴喷丁,用于治疗神经性疼痛的主要药物.这些数据表明上述新型化合物作为用于治疗神经性疼痛的未来药物开发的候选物的巨大潜力.
Doi:10.1021/jm901229S

专利信息

专利号:US-6630602-B1
优先权日:1998-04-16
标题 :Propylisopropyl acetic acid and propylisopropyl acetamide stereoisomers, a method for their synthesis and pharmaceutical compositions containing them
发明人：BIALER MEIR; SPIGELSTEIN OFER; YAGEN BORIS
权利人:YISSUM RES DEV CO
摘要:The present invention relates to racemic propylisopropyl acetic acid and propylisopropyl acetamide and their isomers in their racemic and stereospecific forms, for use in treatment of neurological and psychotic disorders, and affective disorders and to treat pain, headaches and migraines. The isomers are of the compound formula I:wherein R1 is a methyl or ethyl group; R2 is H, methyl or an ethyl group; R3 is ethyl or a propyl group; and R4 is a hydroxyl or amide group; and the total number of carbon atoms in said compound is 8, provided that when R1 is a methyl group and R4 is an amide group, R2 and R3 are not ethyl, further provided that when R1 is an ethyl and R4 a hydroxyl group, only stereoisomers of the compound are referred to. The present invention further relates to a method for the stereoselective synthesis of the 2S and 2R stereoisomer of PID and PIA. The present invention also relates to pharmaceutical compositions containing as an active ingredient a racemic mixture or stereoisomers of the compounds of the general formula (I), which are useful for the treatment of neurological and psychotic disorders, and affective disorders and to treat pain, headaches and migraines.

专利号:US-6969732-B2
优先权日:1999-04-12
标 题 :Propylisopropyl acetic acid and propylisopropyl acetamide stereoisomers, a method for their synthesis and pharmaceutical compositions containing them
发明人：BIALER MEIR; SPIGELSTEIN OFER; YAGEN BORIS
权利人:YISSUM RES DEV CO
摘要:The present invention relates to racemic propylisopropyl acetic acid and propylisopropyl acetamide and their isomers in their racemic and stereospecific forms, for use in treatment of neurological and psychotic disorders, and affective disorders and to treat pain, headaches and migraines. The isomers are of the compound formula I n n R 1 is a methyl or ethyl group; R 2 is H, methyl or an ethyl group; R 3 is ethyl or a propyl group; and R 4 is a hydroxyl or amide group,n nand the total number of carbon atoms in said compound is 8, provided that when R1 is a methyl group and R4 is an amide group, R2 and R3 are not ethyl, further provided that when R1 is an ethyl and R4 a hydroxyl group, only stereoisomers of the compound are referred to.n nn The present invention further relates to a method for the stereoselective synthesis of the 2R stereoisomer of PID and PIA. The present invention also relates to pharmaceutical compositions containing as an active ingredient a racemic mixture or stereoisomers of the compounds of the general formula (I), which are useful for the treatment of neurological and psychotic disorders, and affective disorders and to treat pain, headaches and migraines.

专利号:US-6417399-B1
优先权日:1997-01-14
标 题:Amelioration of neurological disorders by the administration of (2R),(3S), and/or (2S),3(S) stereoisomers of valnoctamide
发明人：BIALER MEIR; YAGEN BORIS; SPIEGELSTEIN OFER; ROEDER MICHAEL; SCHURIG VOLKER
权利人:YISSUM RES DEV CO
摘要:The present invention generally relates to the individual stereoisomers of the drug valnoctamide (a mixture of four stereoisomer kinds, VCD-valmethamide or 2-ethyl-3-methyl pentanamide) useful in treatment of neurological and psychotic disorders such as different kinds of epilepsy and affective disorders, and useful as tranquilizers and to treat pain, and to pharmaceutical compositions containing, as an active ingredient, these stereoisomers. The present invention further relates to a method for stereoselective separation and quantification of the four stereoisomers from a racemic mixture of VCD or plasma of patients treated with the racemic drug. The present invention further relates to a unique method for the synthesis of the individual stereoisomers.

专利号:US-2008214827-A1
优先权日:2004-02-03
标 题:Synthesis of Cyanoimino-Benzoimidazoles
发明人：GOEHRING R RICHARD; WHITEHEAD JOHN; SHAO BIN
权利人:EURO CELTIQUE SA
摘要:Disclosed in certain embodiments is a process for synthesizing a compound of formula (V) and salts thereof.

专利号:US-2002156320-A1
优先权日:2000-01-13
标 题 :Enantioselective synthesis of valproic acid analogues
发明人：NAU HEINZ
摘要:This invention employs camphorsultam as a chiral recoverable auxiliary to provide a new method for manufacturing valproic acid and valproic acid amides that facilitates the enantioselective or diasteroselective production of valproic acid analogs on a larger scale.

专利号:CA-2555219-A1
优先权日:2004-02-03
标 题 :Synthesis of cyanoimino-benzoimidazoles