【药物名称】Dazopride succinate, AHR-5531C(fumarate), AHR-5531D
化学结构式(Chemical Structure):
参考文献No.41886
标题:Synthesis of 4-nitro-1,2-hydrocarbyl pyrazolidines and process for preparation thereof
作者:Lo, Y.S.; Munson, H.R.Jr. (A.H. Robins Co. Inc.)
来源:DE 3130833; FR 2490639; FR 2491065; GB 2081713; JP 3204859; JP 57059868; US 4309552; US 4358599
合成路线图解说明:

An alternative method of producing the 1,2-diethyl-4aminopyrazolidine (VIII) is by reduction of the corresponding nitro compound (VII), which is derived from 1,3-dimorpholino-2-nitropropane (VI) and 1,2-diethylhydrazine (II).

参考文献No.41887
标题:N-(4-Pyrazolidinyl)benzamides and their amino precursors
作者:Cale, A.D.Jr.; Lunsfod, C.D. (A.H. Robins Co. Inc.)
来源:US 4207327
合成路线图解说明:

Dazopride can be prepared by the condensation of the 1,2-diethyl-4-aminopyrazolidine (VIII) with either 4-amino-5-chloro-2-methoxybenzoic acid in the presence of phosphorus trichloride-pyridine or the corresponding mixed anhydride (IX).

参考文献No.41892
标题:Process for the preparation of 4-Pyrazolidinols
作者:Cale, A.D.Jr.; Jenkins, H. (A.H. Robins Co. Inc.)
来源:DE 2031489; ES 380355; FR 2053022; GB 1309018; US 3660426
合成路线图解说明:

The dialkylation of aqueous N,N'-diacetyl-hydrazine by simultaneous addition of diethyl sulfate and potassium hydroxide so as to maintain a pH of 10.5-11.5 affords N,N'-diacetyl-N,N'-diethylhydrazine, which is hydrolyzed to diethylhydrazine (II) by hydrochloric acid. The pH of the acid solution is adjusted to 10, where it is maintained during the addition of epichlorohydrin to give 1,2-diethyl-4-pyrazolidinol (III). The pyrazolidinol is converted to 1,2-diethyl 4-aminopyrazolidine (VIII) by either amination of the corresponding chloro compound (IV) or displacement of the mesyloxy group in compound (V) by the azide ion, followed by reduction.

参考文献No.68107
标题:Dazopride succinate
作者:Cale, A. Jr.
来源:Drugs Fut 1985,10(7),553
合成路线图解说明:

The dialkylation of aqueous N,N'-diacetyl-hydrazine by simultaneous addition of diethyl sulfate and potassium hydroxide so as to maintain a pH of 10.5-11.5 affords N,N'-diacetyl-N,N'-diethylhydrazine, which is hydrolyzed to diethylhydrazine (II) by hydrochloric acid. The pH of the acid solution is adjusted to 10, where it is maintained during the addition of epichlorohydrin to give 1,2-diethyl-4-pyrazolidinol (III). The pyrazolidinol is converted to 1,2-diethyl 4-aminopyrazolidine (VIII) by either amination of the corresponding chloro compound (IV) or displacement of the mesyloxy group in compound (V) by the azide ion, followed by reduction.

合成路线图解说明:

An alternative method of producing the 1,2-diethyl-4aminopyrazolidine (VIII) is by reduction of the corresponding nitro compound (VII), which is derived from 1,3-dimorpholino-2-nitropropane (VI) and 1,2-diethylhydrazine (II).

合成路线图解说明:

Dazopride can be prepared by the condensation of the 1,2-diethyl-4-aminopyrazolidine (VIII) with either 4-amino-5-chloro-2-methoxybenzoic acid in the presence of phosphorus trichloride-pyridine or the corresponding mixed anhydride (IX).

参考文献No.700050
标题:Synthetic and pharmacological properties of N-(1,2-dialkyl-4-pyrazolidinyl)benzamides - Selective gastric prokinetic agents
作者:Munson, H.R. Jr.; Cale, A.D. Jr, Lo, Y.S.; Lunsford, C.D.
来源:187th ACS Natl Meet (April 8-13, St. Louis) 1984,7(9),650
合成路线图解说明:

The dialkylation of aqueous N,N'-diacetyl-hydrazine by simultaneous addition of diethyl sulfate and potassium hydroxide so as to maintain a pH of 10.5-11.5 affords N,N'-diacetyl-N,N'-diethylhydrazine, which is hydrolyzed to diethylhydrazine (II) by hydrochloric acid. The pH of the acid solution is adjusted to 10, where it is maintained during the addition of epichlorohydrin to give 1,2-diethyl-4-pyrazolidinol (III). The pyrazolidinol is converted to 1,2-diethyl 4-aminopyrazolidine (VIII) by either amination of the corresponding chloro compound (IV) or displacement of the mesyloxy group in compound (V) by the azide ion, followed by reduction.

合成路线图解说明:

Dazopride can be prepared by the condensation of the 1,2-diethyl-4-aminopyrazolidine (VIII) with either 4-amino-5-chloro-2-methoxybenzoic acid in the presence of phosphorus trichloride-pyridine or the corresponding mixed anhydride (IX).

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