780004-06-0Relevant articles and documents
Melphalan intermediate and preparation method thereof
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, (2019/08/02)
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.
Sequential C-N and C-O bond formation in a single pot: Synthesis of 2 H -benzo[ b ][1,4]oxazines from 2,5-dihydroxybenzaldehyde and amino acid precursors
Iqbal, Javed,Tangellamudi, Neelima D.,Dulla, Balakrishna,Balasubramanian, Sridhar
, p. 552 - 555 (2012/03/11)
Functionalized β-aryl alanine ester derivatives were found to undergo rapid C-N and C-O bond formation with quinol carbonyl compounds to afford 2H-benzo[b][1,4]oxazines in good to excellent yields. This unprecedented finding reported herein offers a straightforward, highly efficient, and rapid method for the synthesis of 2H-benzo[b][1,4]oxazines.
Efficient synthesis of α-substituted amino acid ester: Alkylation and hydrogenation removal of Schiff's base protecting group
Ansari, Aslam M.,Ugwu, Sydney O.
, p. 2330 - 2340 (2008/09/21)
A general and efficient synthetic route to α-amino acids by alkylation of the sodium salt of Schiff base ester 1 has been described previously. The α-substituted ethyl glycinates 4a-g are prepared in excellent yield by a two-step sequence involving regios
PROCESS FOR THE PREPARATION OF PHENYLALANINE ENAMIDE DERIVATIVES
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Page 45, (2010/02/06)
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).
Melphalan derivatives and their use as cancer chemotherapeutic drugs
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, (2008/06/13)
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.
Compounds and their use in medicine, process for their preparation and pharmaceutical compositions containing them
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Page 21-22, (2008/06/13)
The present invention relates to novel antidiabetic, hypolipidemic, antiobesity and hypocholesterolemic compounds of formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them.
Ethyl N-(diphenylmethylene)glycinate as anionic glycine equivalent. Monoalkylation, dialkylation and michael additions under solid-liquid phase-transfer catalysis
Lopez, Anna,Moreno-Manas, Marcial,Pleixats, Roser,Roglans, Anna,Ezquerra, Jesus,Pedregal, Concepcion
, p. 8365 - 8386 (2007/10/03)
Ethyl N-(diphenylmethylene)glycinate, 1, undergoes monoalkylations, dialkylations and Michael additions to ethylenic and acetylenic acceptors under appropriate solid-liquid phase transfer catalysis conditions. Further transformations of the α-disubstituted ketimines lead to α-alkylated aspartic and glutamic acid derivatives 10, 15, 19 and 26, to bicyclic amino acids or derivatives featuring pyrazolone and isoxazolone moieties 30 and 33, and to α-substituted (E)-3,4-dehydroglutamic acids. Copyright
Synthesis of α-substituted and α,α-disubstituted α-amino acids by controlled mono- and dialkylation of ethyl N-diphenylmethyleneglycinate
Ezquerra,Pedregal,Moreno-Manas,Pleixats,Roglans
, p. 8535 - 8538 (2007/10/02)
Ethyl N-diphenylmethyleneglycinate reacts with one equivalent of alkylating agents in the presence of powdered potassium carbonate to afford, after hydrolysis, monoalkylated glycine esters. A similar process using two equivalents of alkylating agents in t
Improvement in the Enantioselectivity of the Hydrogen Transfer with NADH Models Bearing Amino Alcohols as Chiral Auxiliaries
Cazin, Jacques,Duflos, Jack,Dupas, Georges,Bourguignon, Jean,Queguiner, Guy
, p. 867 - 872 (2007/10/02)
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.
