1711-88-2Relevant articles and documents
C5A RECEPTOR MODULATORS
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Page/Page column 90; 91, (2019/08/08)
The present invention relates to derivatives of formula (I) wherein ring A, X, Y, Z, R1, R2, R3 and R4 are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as C5a receptor modulators.
Amicarbazone synthesis method
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Paragraph 0016; 0017; 0018, (2017/10/07)
The invention discloses an amicarbazone synthesis method, which comprises: synthesizing tert-butyl isocyanate; synthesizing 5-methyl-1,3,4-oxadiazol-2(3H)-one; synthesizing 4-amino-3-isopropyl-5-oxo-1-H-1,2,4-triazole (triazolinone); adding hydrazine hydrate and a second NaOH solution to a third reactor, uniformly stirring, heating to a temperature of 90-100 DEG C, adding the prepared 5-methyl-1,3,4-oxadiazol-2(3H)-one in a dropwise manner, carrying out a reaction after completing the adding, cooling to a room temperature, adding a second solvent, adjusting the pH value to a neutral pH value, freezing for 2-2.5 h, filtering, washing the filter cake, re-crystallizing, and drying to obtain triazolinone; and synthesizing the amicarbazone, wherein triazolinone, potassium hydroxide, a second catalyst and a third solvent are added to a fourth reactor, the prepared tert-butyl isocyanate is added in a dropwise manner, and a heating reaction is performed to obtain the amicarbazone. According to the present invention, the synthesis method has advantages of mild reaction conditions, no requirement of special equipment, good economy, high total yield and good industrial prospect.