541508-62-7Relevant articles and documents
(3aS, 6aR)-1, 3-dibenzyl-tetrahydro -4H-thieno [3, 4-d] imidazole -2, 4-(1H)-dione simple method for preparing
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, (2016/12/01)
The invention relates to a simple preparation method for (3aS,6aR)-1,3-dibenzyl-tetrahydro-4H-thieno[3,4-d]imidazole-2,4-(1H)-dione. The method comprises the following steps: with L-cysteine methyl/ethyl ester hydrochloride as a starting raw material, carrying out N-benzyl protection, ester group reduction and mercapto protection so as to obtain (R)-2-benzylamino-3-acetylmercapto-propanol; then carrying out oxidation with sulfur trioxide-pyridine so as to prepare aldehyde; reacting aldehyde with benzylamine and sodium cyanide so as to prepare (2R,2S),(3R)-dibenzylamino-4-acetylmercapto-n-butyronitrile; carrying out amidation and deprotection cyclization so as to obtain (3aS,6aR),(3aR,6aR)-1,3-dibenzyl-tetrahydro-4H-thieno[3,4-d]imidazole-2,4-(1H)-dione; and carrying out thermal arrangement so as to obtain (3aS,6aR)-1,3-dibenzyl-tetrahydro-4H-thieno[3,4-d]imidazole-2,4-(1H)-dione. The method has the advantages of cheap and easily available raw materials, easily operable reaction conditions, high reaction selectivity, low cost and applicability for industrial production.
INTERMEDIATE FOR BIOTIN AND PROCESS FOR PRODUCING THE SAME
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Page 21, (2008/06/13)
The present invention is to provide a process for preparing a synthetic intermediate of biotin which is industrially advantageous, and discloses a process for preparing a compound represented by the formula (I) : ???wherein R1 and R2 may be the same or different from each other, and each represents hydrogen atom, a benzyl group which may have a substituent(s) on the benzene ring, a benzhydryl group which may have a substituent(s) on the benzen ring, or a trityl group which may have a substituent(s) on the benzene ring, R3 represents cyano group, carboxyl group, an alkoxycarbonyl group, an alkylthiocarbonyl group, or a carbamoyl group which may have a substituent, or a salt thereof which comprises subjecting a compound represented by the formula (II-a) : ???wherein the symbols have the same meanings as defined above, or a salt thereof to ring transformation.