42399-40-6Relevant articles and documents
High-performance liquid chromatography method for assay of diltiazem hydrochloride and its related compounds in bulk drug and finished tablets
Lacroix,Beaulieu,Cyr,Lovering
, p. 243 - 246 (1989)
The method provides for the resolution of trans-diltiazem and seven known and several unknown related compounds from diltiazem HCl. Minimum detectable amounts were 0.1%, except for an intermediate which originates early in the synthetic process, for which the sensitivity is ~2%. The relative standard deviation of the assay procedure is 0.15%. Total related compounds in four bulk drugs and four tablet samples were 0.25%. The specific rotation of four samples of diltiazem HCl analyzed in duplicate was between +112 and +114°. The UV absorption spectra of all compounds exhibited two maxima, one between 203 and 213 nm and the other between 230 and 244 nm.
Synthesis of potential drug metabolites by a modified Udenfriend reaction
Slavik, Roger,Peters, Jens-Uwe,Giger, Rudolf,Bürkler, Markus,Bald, Eric
experimental part, p. 749 - 752 (2011/03/21)
The scope and the limitations of a modified Udenfriend reaction for the one-step synthesis of potential drug metabolites were explored. Several drugs (clozapine, chlorpromazine, imipramine, buspirone, diltiazem, and propranolol) were subjected to modified Udenfriend conditions (Fe2+/Mn 2+/EDTA/ascorbic acid/O2). From each reaction, one to four oxidation products were obtained in 1-8% overall yield. Many of these products (9 out of 14) have been reported to be metabolites of the parent drugs in vivo. The products resulted mainly from aromatic hydroxylation, and are not readily accessible by conventional synthesis. Thus, the described reaction may be useful in drug discovery whenever a facile synthetic access is more important than high yields (e.g., for a fast derivatisation of compounds or the preparation of metabolites). Poorly water-soluble compounds cannot be converted, which is an important limitation of this method. 2010 American Chemical Society.
PROCESS FOR PREPARING DILTIAZEM USING A HETEROGENEOUS TRIFUNCTIONAL CATALYST
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Page 7, (2008/06/13)
The present invention comprises a simplified synthesis of (+)-diltiazem through IE-PdOsW wherein IE is ion-exchanger, catalyzed three-component coupling reaction and Fe3+-exchanged clay catalyzed ring opening of sulfite with 2-aminothiophenol followed by cyclization as key steps.