67630-01-7Relevant academic research and scientific papers
Synthesis method of melphalan
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Paragraph 0057-0060, (2018/06/15)
The invention discloses a synthesis method of melphalan. The synthesis method comprises the following steps: (a), carrying out a reduction reaction: taking a compound which has a structure shown as aformula I as a raw material, and carrying out reduction reaction on the compound, a catalyst and hydrogen to obtain a reduction product shown in formula I, wherein in the formula I, X represents one of oxygen or nitrogen; R1 represents one of hydrogen, saturated alkyl group or unsaturated alkyl group; R2 and R3 respectively represent one of the hydrogen, alkyl carbonyl, amino carbonyl or alkoxycarbonyl; carrying out alkylation reaction on an alkylating reagent and the obtained reduction product in the presence of an acid binding agent to obtain an alkylated product; carrying out hydrolysis reaction on the alkylated product in acid or alkali; after concentrating, adjusting a pH value, extracting, washing and carrying out salification in dried alcohol or ester solvents of hydrochloric acid;then refining with acetonitrile to obtain melphalan hydrochloride. The synthesis method of the melphalan, disclosed by the invention, has the advantages of high yield in each step, simple operation, mild reaction conditions, no high-toxic or high-corrosion reagent, high purity of the obtained product and suitability for industrialized production.
Deuterium-substituted 3-(methylsulfonyl)-L-phenylalanine derivative and medicine composition, medicine preparation and application thereof
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Paragraph 0036; 0111; 0112, (2017/08/31)
The invention provides a deuterium-substituted 3-(methylsulfonyl)-L-phenylalanine derivative and a medicine composition, a medicine preparation and application thereof. The deuterium-substituted 3-(methylsulfonyl)-L-phenylalanine derivative has a structure shown in a formula I. A compound provided by the invention and the derivative thereof have good LFA-1 antagonistic activity, excellent pharmacodynamics property and lower toxicity. The formula I is shown in the description, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20 and R21 are respectively and independently hydrogen or deuterium, and at least contain one deuterium; R is hydrogen.
Fluorescent amino acid derivatives
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Page/Page column 8-9, (2011/04/26)
The subject of the present invention is to provide a fluorescent substance excitable under visible light, having higher photostability and a long fluorescence lifetime. Another subject is to provide a fluorescent substance consists of a non-natural amino
VLA-4 ANTAGONISTS
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Page/Page column 18, (2008/06/13)
Substituted N-[N-(sulphonylphenyl)sulfonyl-prolyl]-phenylalanine derivatives of the present invention are antagonists of the VLA-4 integrin and are useful in the treatment, prevention and suppression of diseases mediated by VLA-4-binding and cell adhesion and activation. Moreover, the compounds of the present invention demonstrate significant receptor occupancy of VLA-4 bearing cells after oral administration and are suitable for once-, twice-, or thrice-a-day oral administration. This invention also relates to compositions containing such compounds and methods of treatment using such compounds.
VLA-4 ANTAGONISTS
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Page/Page column 18-19, (2008/06/13)
Compounds of Formula I are antagonists of VLA-4, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of inflammatory bowel disease including ulcerative colitis and Crohn’s disease, multiple sclerosis, asthma, and rheumatoid arthritis.
NOVEL PHENYLALANINE DERIVATIVE
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Page 40, (2010/02/08)
Phenylalanine derivatives of the following formula, analogues thereof and pharmaceutically acceptable salts thereof have an antagonistic activity to α4 integrin. They are used as therapeutic agents or preventive agents for various diseases concerning α4 i
N-acylamino acid amide compounds and intermediates for preparation thereof
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, (2008/06/13)
The present invention discloses the compound represented by the formula (I): wherein A represents the following formula (a-1) or the following formula (a-2): B represents the following formula (b): (wherein the symbols are each as defined in the specification) or a pharmaceutically acceptable salts thereof, and intermediates for the preparation thereof, which have excellent platelet aggregation inhibitory activity and other properties and useful as prophylactic or therapeutic agents for diseases associated with a fibrinogen receptor, thrombosis, infarction and the like.
Modulation of melphalan resistance in glioma cells with a peripheral benzodiazepine receptor ligand-melphalan conjugate
Kupczyk-Subotkowska, Lidia,Siahaan, Teruna J.,Basile, Anthony S.,Friedman, Henry S.,Higgins, Patricia E.,Song, Di,Gallo, James M.
, p. 1726 - 1730 (2007/10/03)
Peripheral benzodiazepine receptors (PBRs) are located on the outer membrane of mitochondria, and their density is increased in brain tumors. Thus, they may serve as a unique intracellular and selective target for antineoplastic agents. A PBR ligand-melph
Studies on analgesic oligopeptides. II. Structure-activity relationship among thirty analogs of a cyclic dipeptide, cyclo(-Tyr-Arg-)
Sasaki,Akutsu,Matsui,Suzuki,Sakurada,Sato,Kisara
, p. 4435 - 4443 (2007/10/02)
Thirty diketopiperazines were synthesized as analogs of cyclo(-Tyr-Arg-). The analgesic activities of these analogs were evaluated after intracerebral administration in mice. In the cyclo(-X-Arg-) series of analogs, cyclo[-Tyr(Et)-Arg-] showed the most po
