- Synthesis method of multi-configuration isoindoline-1-carboxylic acid amino acid compound
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The invention relates to a synthesis method of a multi-configuration isoindoline-1-carboxylic acid amino acid compound. The synthesis method comprises the following steps: under an acidic condition, the isoindoline-1-carboxylic acid amino acid compound of the compound shown in the formula II or the isomer of the isoindoline-1-carboxylic acid amino acid compound is prepared by reacting the compoundshown in the formula I or the isomer of the compound with formaldehyde, wherein the structural formula of the compound shown in the formula I is shown in the specification, the structural formula ofthe compound shown in the formula II is shown in the specification, and in the formula I and the formula II, R is one of H, alkyl, alkoxy, halogen and trifluoromethyl. According to the synthesis method disclosed by the invention, multi-configuration 2-amino-2-phenylacetic acid or benzene ring mono-substituted 2-amino-2-phenylacetic acid is used as an initial raw material, and under an acidic condition, the initial raw materials are reacted with formaldehyde to prepare a product, namely a multi-configuration isoindoline-1-carboxylic acid amino acid compound; compared with the existing synthesismethod, the method has the advantages that the operation steps are simple, the reaction does not need high temperature higher than 100 DEG C, the reaction temperature is mild, the energy consumptionis low, and the yield of the product is up to 82% or above.
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Paragraph 0047-0053; 0152-0157
(2020/10/14)
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- Anti-heparin peptides
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The invention concerns a compound exhibiting an anti-heparin activity, of formula Z Bm ! (AXA)x Bn ! (AXA)y Bo (AXA)z Bp, the diagnostic reagents comprising it and the use of said compound in an in vitro diagnostic test of a medicine for anti-heparin activity.
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- N-arylsulfonyl aryl aza-bicyclic derivatives as potent cell adhesion inhibitors
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Compounds of Formula I are antagonists of VLA-4 and/or alpha4/beta7, 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 AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.
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