1-(hydroxymethyl)-5,5-diphenyl-2-piperidinone 、 氯化亚砜 在
苯 作用下,
以
苯 为溶剂,
反应 16.0h,
以to give 27 g of crude 1-(chloromethyl)-5,5-diphenyl-2-piperidinone as a white solid的产率得到1-(chloromethyl)-5,5-diphenyl-2-piperidinone
参考文献:
名称:
Diphenyl-1-(aminoalkyl)-2-piperidinone and -2-pyrrolidinone derivatives
[EN] DIPHENYL-2-PIPERIDINONE AND -2-PYRROLIDINONE DERIVATIVES HAVING ANTI-CONVULSANT AND NEUROPROTECTIVE ACTIVITY<br/>[FR] DERIVES DE DIPHENYL-2-PIPERIDINONE ET -2-PYRROLIDINONE POSSEDANT UNE ACTIVITE ANTICONVULSIVANTE ET NEUROPROTECTRICE
申请人:FISONS CORPORATION
公开号:WO1995023135A1
公开(公告)日:1995-08-31
(EN) Compounds of formula (I), wherein two of R1, R2, R3 and R4 independently represent phenyl optionally substituted by one or more groups selected from halogen, hydroxy, nitro, amino, C1-6alkyl and C1-6alkoxy; and the ramainder of R1, R2, R3 and R4 independently represent hydrogen or C1-6alkyl; R5 and R6 independently represent hydrogen, C1-6alkyl or C3-6cycloalkyl, or R5 and R6 together with the nitrogen atom to which they are attached form a C4-6N heterocycle; m is 1 or 2; and n is 1, 2 or 3; and pharmaceutically acceptable acid addition salt thereof; are useful in the treatment of neurodegenerative disorders, particularly epilepsy.(FR) Composés de la formule (I) ainsi que leurs sels d'addition acide acceptables pharmacologiquement, dans laquelle deux parmi R1, R2, R3 et R4 représentent indépendamment phényle facultativement substitué par un ou plusieurs groupes choisis parmi halogène, hydroxy, nitro, amino, alcoyle C1-6 et alcoxy C1-6; et ceux restant parmi R1, R2, R3 et R4 représentent indépendamment hydrogène ou alcoyle C1-6; R5 et R6 représentent indépendamment hydrogène, alcoyle C1-6 ou cycloalcoyle C3-6, ou bien R5 et R6 forment ensemble avec l'atome d'azote auquel ils sont attachés un hétérocycle C4-6N; m vaut 1 ou 2 et n vaut 1, 2 ou 3. Ces composés sont utiles dans le traitement des affections neurodégénératives, notamment dans l'épilepsie.
Diphenyl-1-(aminoalkyl)-2-piperidinone and -2-pyrrolidinone derivatives
申请人:Fisons Corporation
公开号:US05334720A1
公开(公告)日:1994-08-02
Compounds of the formula I, ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 independently represent hydrogen, alkyl, phenyl or substituted phenyl with the proviso that two of R.sub.1, R.sub.2, R.sub.3 or R.sub.4 are phenyl or substituted phenyl and two of R.sub.1, R.sub.2, R.sub.3 or R.sub.4 are hydrogen or alkyl; m represents an integer from 1-2; and n represents an integer from 1-3; or a pharmaceutically acceptable salt thereof. The compounds are useful as pharmaceuticals, in particular, in the treatment of epilepsy.