54777-54-7Relevant academic research and scientific papers
Preparation method of clemastine fumarate
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Paragraph 0066; 0067-0073, (2017/09/01)
The invention relates to a preparation method of clemastine fumarate, which comprises the following steps of: step 1: performing chlorination substitution on hydroxyl by taking N-methyl-2-(2-ethoxyl) pyrrolidine as a starting material to prepare N-methyl-(2-chloroethyl) pyrrolidine, step 2: allowing N-methyl-(2-chloroethyl) pyrrolidine and 1-(4-chlorphenyl)-1-phenyl alcohol to react as raw materials by the action of sodamide to form racemic clemastine and then adding succinic acid to prepare racemic clemastine succinate, step 3: performing splitting by using L-(+)-tartaric acid in acetone and water by taking racemic clemastine succinate as a raw material, adding fumaric acid for salification to form a crude product of clemastine fumarate, and step 4: performing recrystallization on the crude product of clemastine fumarate by using an acetone aqueous solution to form a pure product of clemastine fumarate.
Pyrazolyl derivatives, preparation process and intermediates of this process as medicinal products and pharmaceutical compositions containing them
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Page/Page column 57, (2008/06/13)
The present invention relates to the novel derivatives of formula (I) in which A is, if it is present, a (C1-C6) alkyl, a (C3-C6) alkenyl, a (C3-C6) alkynyl, a (C3-C7) cycloalkyl or a (C5-C7) cycloalkenyl, R1 is an NR6R7, (C4-C7) azacycloalkyl, (C5-C7) azacycloalkenyl, (C5-C9) azabicycloalkyl or (C5-C9) azabicycloalkenyl group; A-R1 is such that the nitrogen of R1 and the nitrogen in the 1-position of the pyrazole are necessarily separated by at least two carbon atoms, R3 is an H, halogen, OH, SH, NH2, ORc, SRc, SORa, SO2Ra, NHCHO, NRaRb, NHC(O)Ra, NHC(S)Ra or NHSO2Ra, R4 is an aryl or heteroaryl; and R5 is an H, halogen, CF3, CHF2, CH2F, linear or branched (C1-C6) alkyl or (C3-C7) cycloalkyl to their racemates, enantiomers and diastereoisomers and to their mixtures, their tautomers and to their pharmaceutically acceptable salts.
