Acetylation Acid activation, diphenyl

Esters of diphenylacetic acids with derivatives of ethanol-amine show mainly the antispasmodic component of the atropine complex of biologic activities. As such they find use in treatment of the resolution of various spastic conditions such as, for example, gastrointestinal spasms. The prototype in this series, adiphenine (47), is obtained by treatment of diphenyl acetyl chloride with diethylaminoethanol. A somewhat more complex basic side chain is accessible by an interesting rearrangement. Reductive amination of furfural (42) results in reduction of the heterocyclic ring as well and formation of the aminomethyltetrahydro-furan (43). Treatment of this ether with hydrogen bromide in acetic acid leads to the hydroxypiperidine (45), possibly by the intermediacy of a carbonium ion such as 44. Acylation of the alcohol with diphenylacetyl chloride gives piperidolate (46). ... 

The proton spectra of 1-substituted 3-nitropyrazoles [296], 5-substituted 3-methyl-l-aryl-4-nitropyrazoles [297, 298], 1,3- and l,5-diphenyl-4-nitropyra-zoles [281], 5-iodo-4-nitro-l,3-dimethylpyrazole [299], l-methyl-3-nitro-4- and l,3-methyl-4-nitro-5-phenylethynylpyrazoles [300], l-methyl-3-nitro-5-methoxy-carbonylpyrazole [301], l-methyl-3-nitro- and l-methyl-5-nitro-4-cyanopyrazoles [302], A-(2,4-dinitrophenyl)nitropyrazoles [303], a- and [3-anomers of 3-nitro-and4-nitropyrazolyl-l-ribonucleosides [304, 305], 3-substituted 1,5-dimethyl- [306] and 5-substituted l,3-dimethyl-4-nitropyrazoles [279], l-acetyl-3-anilino-4-nitro-5-dimethylaminopyrazoles [307], 3-substituted 4-nitro-5-carboxylic acid derivatives [308, 309], 4-nitropyrazolo[4,3-e][l, 4]diazepin-5,8-diones showing antimicrobial activity [310], l-heteryl-4-nitropyrazole derivatives [311], 3-nitro- and 5-nitro-l-methylpyrazole [312], 4-nitro-5-(trimethylsilyl)pyrazole [313], 3-methyl-4-nitro-pyrazol-5-ones [298], and some other nitropyrazoles [248, 314-320] have been examined. 

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