- INTRAMOLECULAR CYCLIZATION OF GUANIDINOALKANETHIOLS IN AQUEOUS SOLUTION
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We have demonstrated the basic possibility of cyclizing guanidinoalkanethiols of different structure to thiazolines and thiazines.The rate of reaction depends on the pH of the medium.The concentration of buffer and the addition of heavy water and α-D,L-alanine have virtually no effect on the rate of reaction.
- Mandrugin, A. A.,Fedoseev, V. M.,Khomutov, S. M.,Rodyunin, A. A.,Leshchev, Yu. A.
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p. 1262 - 1266
(2007/10/02)
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- S-DERIVATIVES OF THIOUREA. XX. REACTION OF THIOUREA WITH TERMINAL DIBROMOALKANES
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The kinetics of the reaction of thiourea with terminal dibromoalkanes Br(CH2)nBr, where n= 1-5, were investigated by radiochromatography.It was established that the reaction of thiourea with 1,4-dibromobutane and 1,5-dibromopentane leads to the formation of only products from substitution of one or two bromine atoms by thiourea.In the case of 1,2-dibromoethane and 1,3-dibromopropane 2-amino-2-thiazoline and 2-amino-5,6-dihydro-4H-1,3-thiazine were found in addition to the analogous substitution products.The rate constants of the individual stages of the processes were determined.A series of S-bromoalkylisothioureas Br(CH2)nSC+.(NH2)2Br-, where n= 2-5, were synthesized.It was shown that the rate of their reaction with thiourea is higher than for terminal dibromoalkanes and (for n= 3-5) alkyl halides Br(CH2)nH.It was found that the reactivity varies irregularly with increases in the length of the polymethylene chain for bromoalkylisothioureas, and this evidently results from the superimposition of several effects from the substituent.
- Tkachenko, S. E.,Sal'nikov, D. I.,Lys, Ya. I.,Fedoseev, V. M.,Zhurilin, V. S.
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p. 878 - 884
(2007/10/02)
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- 2,3-Dihydro-imidazo[2,1-b]-thiazole derivatives and applications thereof
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This invention relates to 2,3-dihydro-imidazo[2,1-b]-thiazole derivatives of the formula: STR1 in which R represents a phenyl or substituted phenyl group, R1 represents a hydrogen atom or a phenyl substituted with a halogen atom or a C1-4 alkoxy group, R2, r3, r4 and R5, which may be the same or different, represent each a hydrogen atom, a C1-4 alkyl group or a phenyl radical, R1, r2, r3, r4 and R5 not being simultaneously hydrogen when R represents a phenyl group or a phenyl group substituted with a halogen atom or a nitro group, and their pharmaceutically acceptable acid addition salts. Said compounds have an anti-inflammatory and analgesic activity.
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