62760-10-5

Upstream product

• 54527-68-3 2-chloroethyl acetoacetate 
• 99-61-6 3-nitro-benzaldehyde 

Downstream Products

• 54851-30-8 2,6-dimethyl-4-(3'-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid 3-β-chloroethyl ester 5-isopropyl ester 
• 91040-32-3 2,6-Dimethyl-4-(3-nitro-phenyl)-1,4-dihydro-pyridine-3,5-dicarboxylic acid 3-(2-chloro-ethyl) ester 5-isobutyl ester 
• 100427-03-0 2,6-Dimethyl-4-(3-nitro-phenyl)-1,4-dihydro-pyridine-3,5-dicarboxylic acid 3-(2-chloro-ethyl) ester 5-(2-propoxy-ethyl) ester 
• 75091-01-9 2-Cyano-6-methyl-4-(3-nitro-phenyl)-1,4-dihydro-pyridine-3,5-dicarboxylic acid 5-{2-[(3,4-dichloro-benzyl)-methyl-amino]-ethyl} ester 3-ethyl ester 
• 74655-11-1 2-Cyano-6-methyl-4-(3-nitro-phenyl)-1,4-dihydro-pyridine-3,5-dicarboxylic acid 5-{2-[(4-chloro-benzyl)-methyl-amino]-ethyl} ester 3-ethyl ester 
• 62760-80-9 2-(N-methyl-N-benzylamino)ethyl 2-methyl-4-(3-nitrophenyl)-5-ethoxycarbonyl-6-hydroxymethyl-1,4-dihydropyridine-3-carboxylate 
• 74654-94-7 2-Diethoxymethyl-6-methyl-4-(3-nitro-phenyl)-1,4-dihydro-pyridine-3,5-dicarboxylic acid 5-{2-[(3,4-dichloro-benzyl)-methyl-amino]-ethyl} ester 3-ethyl ester 
• 74654-93-6 2-Diethoxymethyl-6-methyl-4-(3-nitro-phenyl)-1,4-dihydro-pyridine-3,5-dicarboxylic acid 5-{2-[(4-chloro-benzyl)-methyl-amino]-ethyl} ester 3-ethyl ester 
• 74655-03-1 2-Formyl-6-methyl-4-(3-nitro-phenyl)-1,4-dihydro-pyridine-3,5-dicarboxylic acid 5-{2-[(3,4-dichloro-benzyl)-methyl-amino]-ethyl} ester 3-ethyl ester 
• 74655-02-0 2-Formyl-6-methyl-4-(3-nitro-phenyl)-1,4-dihydro-pyridine-3,5-dicarboxylic acid 5-{2-[(4-chloro-benzyl)-methyl-amino]-ethyl} ester 3-ethyl ester 
• 74655-19-9 2-Cyano-6-methyl-4-(3-nitro-phenyl)-1,4-dihydro-pyridine-3,5-dicarboxylic acid 5-(2-acetoxy-ethyl) ester 3-ethyl ester 
• 75530-90-4 2-hydroxyethyl 2-cyano-3-ethoxycarbonyl-6-methyl-4-(3-nitrophenyl)-1,4-dihydropyridine-5-carboxylate 
• 75090-92-5 2-Formyl-6-methyl-4-(3-nitro-phenyl)-1,4-dihydro-pyridine-3,5-dicarboxylic acid 3-ethyl ester 5-(2-hydroxy-ethyl) ester 
• 62760-16-1 2-hydroxyethyl 2-diethoxymethyl-3-ethoxycarbonyl-6-methyl-4-(3-nitrophenyl)-1,4-dihydropyridine-5-carboxylate 

Relevant academic research and scientific papers

Asymmetric N-(3,3-diphenylpropyl)aminoalkyl esters of 4-aryl-2,6- dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acids with antihypertensive activity

A series of asymmetric 4-aryl-1,4-dihydropyridine-3,5-dicarboxylates characterized by the presence of a 3,3-diphenylpropylamino moiety in one of the ester groups were synthesized. They exhibited remarkable antihypertensive activity in spontaneously hypertensive rats as well as affinity for the 1,4- dihydropyridines binding site labelled by 3H-nitrendipine in the calcium channel. Introduction of this bulky and lipophilic amine confers to the whole series an elevated level of antihypertensive activity and a long duration of action, a structure-dependent modulation of the activity being found only in the subset characterized by the presence of a branched propylene bridge between the ester and the amino groups. The presence of the amino group is essential for oral activity. Out of this series, compound 9u (Rec 15/2375- lercanidipine) was selected for clinical development and obtained marketing authorization as an antihypertensive in several countries.

Studies on nilvadipine. II. Synthesis and structure-activity relationships of 2-hydroxymethyl- and 2-cyano-1,4-dihydropyridines containing heteroatom-substituted ester at the 5-position

The synthesis of new 2-hydroxymethyl- and 2-cyano-1,4-dihydropyridines possessing a heteroatom-substituted alkyl ester group at the 5-position of the nucleus is described. The esters were introduced via a suitable method selected from the modified Hantzsch method (method A), the hydrolysis of a chloroethyl ester obtained by method A (method B) or the replacement of the chlorine atom with various kinds of amino groups (method C). Hydroxymethyl and cyano groups at the 2-position were prepared in a similar manner to that described in a previous paper. The hypotensive activities of the compounds prepared in this paper were compared with the corresponding alkyl ester at the 5-position reported previously. It was found that N-benzylmethylaminoethyl esters, especially N-(4-chlorobenzyl)and N-(3,4-dichlorobenzyl)-N-methylaminoethyl esters, were suitable substituents at the 5-position of the 1,4-dihydropyridine nucleus and that these substituents were somewhat more effective for hypotensive activity than simple alkyl esters in a series of 2-hydroxymethyl-1,4-dihydropyridine derivatives. But it was found that the effect was reversed in a series of 2-cyano-1,4-dihydropyridine derivatives. Both of them were found to be inferior to nilvadipine (1c), accepted in clinical use for the treatment of hypertension.

Carbostyril Derivative

Carbostyril derivative or a pharmaceutically acceptable acid addition salt thereof, having excellent platelate aggregation inhibitory effect, calcium antagonism, hypotensive effect and phosphodiesterase inhibitory effect are useful as prophylactic or treating agents for thrombosis, circulation improving agents for coronary blood flow such as coronary vasodilators, hypotensive agents and phosphodiesterase inhibitors. Furthermore, the carbostyril derivatives are weak in heart rate increasing activity and also in cardiac muscle contraction increasing activity, and the carbostyril derivatives are useful agents for curing and treating heart diseases such as cardiac angina and myocardial infarction caused by hypercoagulability of the platelets. Processes are disclosed for preparation of the carbostyril derivatives.