| 摘要 |
<p>1,225,955. Thien - 2 - ylmethyl esters of amino and N - acylamino acids. FARBWERKE HOECHST A.G. 18 March, 1968 [17 March, 1967], No. 4090/69. Divided out of 1,216,247. Heading C2C. Novel amino- or N-acylamino-acid thien-2- ylmethyl esters, where acyl is defined as any N-acyl protective group known or used in peptide chemistry, are prepared by reacting 2- chloromethylthiophene with an alkali metal or alkylammonium salt of the N-acylamino acid in a solvent at 18-60‹ C. and if required deacylating the N-acylamino acid ester. Specified amino acids are glycine, alanine and leucine and their N-benzyloxycarbonyl, N-t-butyloxycarbonyl and N - o - nitrophenylsulphenyl derivatives. Deacylation is suitably effected with HCl gas in an inert solvent, yielding the amino acid in the form of the hydrochloride. Examples relate to the preparation of the esters of tbutyloxycarbonyl - L - glycine, t - butyloxy - carbonyl - L - leucine, o - nitrophenyl - sulphenyl- L - alanine and o - nitrophenylsulphenyl - L- leucine and the hydrochlorides of the deacylated amino acid esters.</p> |
