摘要:
A process for preparing a tert-alkyl carboxylic acid ester represented by the formula (III): wherein R 1 is an organic group; and each of R 2 and R 3 is independently an alkyl group having 1 to 4 carbon atoms, comprising reacting a carboxylic acid represented by the formula (I):
R 1 -COOH (I)
wherein R 1 is as defined above, with a vinylidene compound represented by the formula (II): wherein R 2 and R 3 are as defined above, in the presence of a phosphorus halide. The tert-alkyl carboxylic acid ester can be used as intermediates for pharmaceuticals such as antibiotics.
摘要:
A series of compounds capable of deriving an intermediate for the production of a compound (A) of the following formula, which is an anti-HIV drug, and a production method thereof. To be specific, 4-(pyridin-2-yl)benzaldehyde hydrazone, a production method of this compound, and a production method from this compound to N-(tert-butoxycarbonyl)-N'-[4-(pyridin-2-yl)phenylmethylidene]hydrazine. In addition, a salt of 2-(4-bromomethylphenyl)pyridine, 2-(4-dibromomethylphenyl)pyridine and a salt thereof, production methods of these compounds, and production methods to derive 4-(pyridin-2-yl)benzaldehyde which is a production intermediate for 4-(pyridin-2-yl)benzaldehyde hydrazone from these compounds.
摘要:
An L-tartrate of a trans-(-)-4-(4-fluorophenyl)-3-hydroxymethylpiperidine compound, represented by the formula (I): wherein R 1 is hydrogen atom, a substituted or unsubstituted, linear or branched alkyl group having 1 to 6 carbon atoms, or an aralkyl group having 7 to 12 carbon atoms. The L-tartrate of trans-(-)-4-(4-fluorophenyl)-3-hydroxymethylpiperidine compound can be suitably used as an intermediate for pharmaceuticals such as paroxetine which is useful, for example, as an antidepressant.
摘要:
A method for producing alkylated cyanoacetylurea from an easily obtainable starting material An industrially available cyanoacetylurea and a carbonyl compound are reacted in a polar solvent under reducing conditions to alkylate cyanoacetylurea In addition, a reaction of cyanoacetylurea and acetone under reducing conditions affords isopropylation of cyanoacetylurea.
摘要:
A process for preparing a 2-cyanobiphenyl compound represented by the formula (II): wherein R 1 is an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms, or hydrogen atom, from a phenylmagnesium chloride compound represented by the formula (I): wherein R 1 is as defined above. According to the process, a 2-cyanobiphenyl compound represented by the formula (II) can be economically, simply, industrially and advantageously prepared.
摘要:
A process for preparing a 2-cyanobiphenyl compound represented by the formula (II): wherein R 1 is an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms, or hydrogen atom, from a phenylmagnesium chloride compound represented by the formula (I): wherein R 1 is as defined above. According to the process, a 2-cyanobiphenyl compound represented by the formula (II) can be economically, simply, industrially and advantageously prepared.
摘要:
A piperidine derivative, which can be used as an intermediate for pharmaceuticals such as paroxetine useful as antidepressants, represented by the general formula (I): wherein R 1 is hydrogen atom, benzyloxycarbonyl group or tert-butoxycarbonyl group; R 2 is hydroxymethyl group, an alkylsulfonyloxymethyl group having an alkyl moiety of 1 to 2 carbon atoms, phenylsulfonyloxymethyl group which may have methyl group at the 4-position, (3,4-methylenedioxyphenyl)oxymethyl group, carboxyl group or -CO 2 R 7 group in which R 7 is an alkyl group having 1 to 5 carbon atoms, and Z is methylene group or carbonyl group, with proviso that, (A) when R 1 is benzyloxycarbonyl group or tert-butoxycarbonyl group, then R 2 is hydroxymethyl group, an alkylsulfonyloxymethyl group having an alkyl moiety of 1 to 2 carbon atoms, phenylsulfonyloxymethyl group which may have methyl group at the 4-position or (3,4-methylenedioxyphenyl)oxymethyl group, and Z is methylene group; or (B) when R 1 is hydrogen atom and Z is carbonyl group, then R 2 is carboxyl group or -CO 2 R 7 group (R 7 is as defined above); or (C) when R 1 is hydrogen atom and Z is methylene group, then R 2 is hydroxymethyl group. Also processes for the production of the intermediates are described.
摘要:
The present invention is directed to a method for producing a 2-amino-6-halogenopurine, a novel synthesis intermediate therefor and a method for producing said synthesis intermediate. The desired 2-amino-6-halogenopurine is an intermediate for the production of the compound useful as an antiviral agent, and by using the compound of the present invention as a starting material, the 2-amino-6-halogenopurine can be produced with high yield.