140171-49-9Relevant academic research and scientific papers
Process for making amlodipine
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, (2008/06/13)
Amlodipine and related analogues thereof are prepared by the following general reaction scheme: R1and R2each independently represent a C1-C4alkyl group. The process provides for the formation of compounds of formula (1) in good yield and purity. Further, the compounds of formula (1) can be used as calcium channel blockers or as reference standards or reference markers for checking the purity of amlodipine.
Process for making amlodipine, derivatives therof, and precursors therefor
-
, (2008/06/13)
Amlodipine and related analogues thereof are prepared by the following general reaction scheme: R1 and R2 each independently represent a C1-C4 alkyl group. The process provides for the formation of compounds of formula (1) in good yield and purity. Further, the compounds of formula (1) can be used as calcium channel blockers or as reference standards or reference markers for checking the purity of amlodipine.
Long-acting dihydropyridine calcium antagonists. 9. Structure activity relationships around amlodipine
Alker, D,Arrowsmith, JE,Campbell, SF,Cross, PE
, p. 907 - 913 (2007/10/02)
The preparation of a range of 1,4-dihydropyridine analogues of amlodipine has been undertaken and their calcium antagonist activities on rat aorta have been evaluated.Increasing the size of the C5 ester group dramatically reduces calcium antagonist activity, a trend which would be compatible with the carbonyl group of that ester binding to the DHP receptor.Amlodipine analogues with extended C3 ester substituents also have lower potency than amlodipine, possibly because of disruption of a favourable interaction between the protonated amino group on the 2-substituentand the DHP receptor.Replacement of the 6-methyl substituent in amlodipine by alkoxyalkyl groups or electron-withdrawing groups is also detrimental to calcium antagonist activity. amlodipine / 1,4-dihydropyridine / structure activity relationship
