Banyu Pharmaceutical Co. Ltd

Nobuo Harada

Kunio Suzuki

Tetsuji Miyano

Kiyofumi Ishikawa

Mitsuo Yano

Ikuo Matsumoto

Junji Yoshizawa

A process for preparing a 2-carbamoyloxyalkyl-1,4-dihydropyridine derivative represented by the general formula: ##STR1## which comprises: (a) reacting a 3-amino-3-carbamoyloxyalkylacrylic acid derivative represented by the general formula: ##STR2## with a benzylidene compound represented by the general formula: ##STR3## (b) reacting the 3-amino-3-carbamoyloxyalkylacrylic acid derivative of the general formula II with an aldehyde compound represented by the general formula: ##STR4## and a .beta.-keto-ester compound represented by the general formula:

3-amino-3-carbamoyloxyalkylacrylic acid intermediates to dihydropyridines

An .alpha.-tocopheryl 5-substituted picolinate of the formula ##STR1## wherein R represents an alkyl group which may have a substituent, a lower alkenyl group, a phenyl(lower alkyl) group, or a phenyl group which may have a substituent, and Q represents a methylene group or an oxygen or sulfur atom, or a pharmaceutically acceptable acid addition salt thereof. This compound can be produced by reacting a substituted picolinic acid of the formula ##STR2## wherein R and Q are as defined above, or its reactive derivative with .alpha.-tocopherol of the formula ##STR3## and as required, contacting the resulting compound with a pharmaceuticlly acceptable acid. A pharmaceutical composition comprising said compound as an active ingredient is useful for the treatment of hypertension.

.alpha.-Tocopheryl ester of 5-substituted picolinic acid and hypotensive

Novel compounds having vasodilation and hypotensive effects are represented by the formula ##STR1## where R.sup.1 is halogen, nitro, cyano or lower alkoxy; each of R.sup.2 and R.sup.3 is lower alkyl, lower haloalkyl, lower alkoxyalkyl, aralkyloxyalkyl, aryloxyalkyl, lower alkenoxyalkyl, N,N-di-lower alkylaminoalkyl, N-lower alkyl-N-aralkylaminoalkyl, piperidylalkyl, 4-lower alkyl piperazinylalkyl, norpholinoalkyl or 1-pyrrolidinylalkyl; R.sup.4 is lower alkyl; A is lower alkylene; and R.sup.5 is hydrogen, lower alkyl, cycloalkyl of 3 to 7 carbon atoms, or aryl unsubstituted or substituted by one or two substituents selected from halogen, nitro, lower alkyl, lower alkoxy, di-lower alkylamino and cyano. Also disclosed are processes for their preparation.

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Okazaki, Japan

Nobuo Harada