Antihypertensives ACE inhibitors

CENTRALLY ACTING ANTIHYPERTENSIVES ACE INHIBITORS Some evidence that when switching from donidine to captopril, there may be a delayed onset of action of captopril Sudden cessation of donidine causes rebound t BP, and this may be the reason for the delay in onset of captopril Monitor BP at least weekly until stable... 

Captopril (101) is an antihypertensive ACE inhibitor. Syntheses of note involve classical resolution of the acetyl ff-mercaptoisobutyric acid to provide the (/ )-enantiomer (102) [126], and secondly, generation of the isobutyrate component following the asymmetric hydroxylation of isobutyric acid by a microbial strain [127] Scheme 5.41). The important point is to have the isobutyrate component resolved prior to the coupling with proline, so that the proline is fully utilized. 

Enalapril [75847-73-3], antihypertensive (ACE inhibitor), 93. In one method, phosgene is used to activate L-alanine 89 as its N-carboxy anhydride (NCA) 90, which is then used to acylate the L-proline 91 affording the semisynthetic dipeptide Ala-Pro 92 [68], Processes based on the reaction of activated derivatives of N-[1(S)-ethoxycarbonyl-3-phenylpropyl]-L-alanine with L-proline have also been reported [69-71]. 

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