Abstract:
:The synthesis of diazoketone analogs of amino acids and associated problems were investigated with N-phthaloyl-DL-alanine serving as a model. The carboxyl was activated by conversion to the acid chloride or, under mild conditions, to the mixed anhydride obtained with ethyl chloroformate or dicyclohexylcarbodiimide; the product was reacted with diazomethane. Deblocking the phthaloyl group with hydrazine gave 3-amino-1-diazo-2-butanone as a well-characterized solid salt and as a less stable oil. Further reactions of the blocked diazoketone of DL-alanine, such as conversion to alpha-haloketones, Wolff rearrangement, and deuterium exchange on C-1 were investigated. 3-A-mino-1-diazo-2-butanone had moderate inhibitory activity against mouse mammary adenocarcinoma in cell culture.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Paul B,Korytnyk Wdoi
10.1002/jps.2600670518subject
Has Abstractpub_date
1978-05-01 00:00:00pages
642-5issue
5eissn
0022-3549issn
1520-6017pii
S0022-3549(15)41997-5journal_volume
67pub_type
杂志文章abstract::In this study the relationships between previously reported connectivity indices described by Kier and Hall and steric contributions to the rate constants for several series of reactions are examined. Rate data were examined for four different series of reactions, which were chosen to represent a range of different re...
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abstract::When heated at temperatures in excess of 100 degrees, the stability of neomycin in aqueous ophthalmic formulations was improved by the addition of edetate disodium (0.01%). As the exposure temperature was reduced, the degree of stability enhancement diminished until the effect was reversed, and addition of edetate dis...
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journal_title:Journal of pharmaceutical sciences
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journal_title:Journal of pharmaceutical sciences
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