59156-43-3Relevant academic research and scientific papers
4H-3,1-BENZOXAZIN-4-ONE COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE INHIBITION OF SERINE PROTEASES
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, (2008/06/13)
A 4H-3,1-benzoxazin-4-one compound of the formula (I): STR1 wherein R is a hydrogen atom or alkyl radical, A is an amino acid residue or a peptide having 2 to 3 amino acid residues, which amino acid residue may have a side chain thereof protected by a protective radical, X is an alkyl, fluoroalkyl, OR 1 or NHR 1 radical wherein R 1 is an alkyl radical, and Y is a protective radical for an amino radical, and salts thereof, exhibit an excellent inhibitory activity against serine proteases, especially against human leukocyte elastase, and thus are useful as an effective component of a medicine for inhibiting elastase.
Preparation of Some Acetylated, Reduced and Oxidized Derivatives of 2,4-Diaminotoluene and 2,6-Dinitrotoluene
Mori, Masa-aki,Inoue, Masami,Nunozawa, Tetsuji,Miyahara, Tatsuro,Kozuka, Hiroshi
, p. 4859 - 4861 (2007/10/02)
4-Acetylamino-2-hydroxylaminotoluene (4AA2HAT) and 2-hydroxylamino-6-nitrotoluene (2HA6NT) were prepared from 4-acetylamino-2-nitrotoluene (4AA2NT) and 2,6-dinitrotoluene (2,6-DNT), respectively, by reduction with zinc dust and NH4Cl. 2,6-Dinitrobenzylalcohol (2,6-DNB) and 2,6-dinitrobenzoic acid (2,6-DNBA) were prepared from 2,6-dinitrobenzaldehyde (2,6-DNBAl) by reduction with NaBH4 and by oxidation with KMnO4, respectively. 2-Acetylamino-4-aminobenzoic acid (2AA4ABA) was prepared from 4-nitroanthranilic acid (4NAA) by acetylation followed by reduction with NaBH4 and Pd-C. 2,4-Diacetylaminobenzoic acid (2,4-DAABA) was prepared from 4NAA by reduction with NaBH4 and Pd-C followed by acetylation. 4-Acetylamino-2-aminobenzoic acid (4AA2ABA) was prepared from 4NAA by reduction and acetylation followed by chelation with Cu(AcO)2.Keywords- 4-acetylamino-2-hydroxylaminotoluene; 2-hydroxylamino-6-nitrotoluene; 2,6-dinitrobenzylalcohol; 2,6-dinitrobenzoic acid; 2-acetylamino-4-aminobenzoic acid; 4-acetylamino-2-aminobenzoic acid; 2,4-diacetylaminobenzoic acid; carcinogenicity; mutagenicity; preparation
