| 摘要 |
<p>1308826 2,4-Thiazolidinedicarboxylic acid derivatives FERLUX 3 June 1970 [5 June 1969 9 March 1970] 26825/70 Heading C2C [Also in Division A5] The invention comprises novel 2,4-thiazolidinedicarboxylic acid derivatives of the formula wherein R 1 is OH and R 2 is 2-trimethylammonio-ethoxy (as chloride), 2-mercaptoethylamino, 1 - carboxy - 3 - (methylthio)propylamino, 3-pyridylmethoxy, and 1-carboxy-4- guinidinobutylamino, and where R 2 is H and R 1 is carboxymethylamino, 2-mercaptoethylamino, and the magnesium, betaine and arginine salts of 2,4-thiazolidinedicarboxylic acid, and their preparation. The compounds are obtained by reacting glyoxylic acid or esters or amides thereof with 2-amino-3-mercaptopropionic acid hydrochloride or esters or amides thereof in mixtures of suitable solvents at about 20‹ C. in the presence of sodium or potassium acetate or triethylamine. 2,4-Thiazolidinedicarboxylic acid is obtained by reacting L-cysteine hydrochloride monohydrate with glyoxylic acid, followed by, if desired or necessary, esterification and/or amidification. The following intermediates are also prepared: [2 - Amino - 3 - (benzylthio)propionyl]- glycine, [2 - amino - 3 - mercaptopropionyl]- glycine, N - (benzylthioethyl) - 2 -amino - 3- (benzylthio)propionamide, 2 - amino - N - (2- mercaptoethyl) - 3 - mercaptopropionamide, 3- pyridylmethyl glyoxylate, N - (2 - mercaptoethyl)glyoxylamide, N - [1 - carboxy - 3- (methylthio)propyl]glyoxylamide, and N - (1- carboxy-4-guanidinobutyl)glyoxylamide.</p> |
