- Melphalan intermediate and preparation method thereof
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The invention discloses a Melphalan intermediate and a preparation method thereof. The Melphalan intermediate is prepared by acidifying a compound p-nitrobenzaldehyde under the action of methanol, a hydrochloric acid solvent, etc. The preparation method has a route with mild reaction conditions, is higher than an existing preparation method in yield, is economical and effective, and is suitable for large-scale industrial production. The synthesis route is as shown in the description.
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- PROCESS FOR THE PREPARATION OF PHENYLALANINE ENAMIDE DERIVATIVES
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A process for the preparation of a class of phenylalanine enamide derivatives is described formula (1) wherein: Ar1 is an optionally substituted aromatic or heteroaromatic group; L2 is a linker group selected from -N(R4)- [where R4 is a hydrogen atom or an optionally substituted straight or branched C1-6alkyl group], -CON(R4)-, or -S(O)2N(R4)-; R1 is a carboxylic acid (-CO2H) or a derivative or biostere thereof; R2 is a hydrogen atom or a C1-6alkyl group; Rx, Ry and Rz which may be the same or different is each an atom or group -L1(Alk1)n(R3)v; and the salts, solvates, hydrates and N-oxides thereof; which comprises reacting a compound of formula (2): wherein: Qa is a group -N(R4)H; and the salts, solvates, hydrates and N-oxides thereof; with a compound Ar1W wherein W is a group selected from X1 (wherein X1 is a leaving atom or group), -COX2 (wherein X2 is a halogen atom or a -OH group) or -SO2 X3 (in which X3 is a halogen atom).
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- Melphalan derivatives and their use as cancer chemotherapeutic drugs
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The invention refers to new alkylating di- and tripeptides based on a melphalan unit, and one or two additional amino acids or amino acid derivatives, which can be used in the treatment of carcinogenic diseases. Further, the invention refers to a a pharmaceutical composition comprising the alkylating peptides of the invention.
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- Improvement in the Enantioselectivity of the Hydrogen Transfer with NADH Models Bearing Amino Alcohols as Chiral Auxiliaries
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Chiral amino alcohols have been linked to the γ-carbonyl group of the 5,7-dihydrothienopyridines (4a-d).These models are much more easily handled in mild conditions than common NADH models.The factors affecting enantiomeric excess have been studied, e.g. influence of temperature, polarity of solvents, magnesium concentration, and hydrogen bonding.By appropriate modifications of the chiral auxiliary, the rigidity of the ternary complex: model-Mg2+-substrate involved has been enhanced.In this way a high enantiomeric excess has been obtained.
- Cazin, Jacques,Duflos, Jack,Dupas, Georges,Bourguignon, Jean,Queguiner, Guy
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p. 867 - 872
(2007/10/02)
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