- Lesinurad intermediate impurity dimer as well as preparation method and application thereof
-
The invention relates to a Lesinurad intermediate impurity dimer as well as a preparation method and application thereof, and belongs to the technical fields of drug synthesis and analysis. In order to solve the problem that an impurity in the synthesis process cannot be effectively identified, the invention provides the Lesinurad intermediate impurity dimer as well as the preparation method and application of the dimer. The preparation method of the dimer comprises the following steps: performing a reaction on 4-cyclopropyl-1-naphthyl isothiocyanate and formylhydrazine to obtain a compound containing the impurity dimer represented by a formula III shown in the description, and performing column chromatography separation to obtain the corresponding dimer or performing a reaction on 4-cyclopropyl-1-naphthyl isothiocyanate and hydrazine to obtain the impurity dimer. The impurity dimer provided by the invention can provide analysis and monitoring for the impurity in the synthesis processof an intermediate, effectively provide a reference substance of the impurity, facilitates improving the quality of the Lesinura intermediate and the product, and facilitates improving the product yield and production efficiency; and the process is simple and easy to operate.
- -
-
Paragraph 0031-0032; 0034; 0036; 0041
(2018/11/27)
-
- Optically pure thioacetic compound
-
The invention belongs to the field of pharmacy and relates to an optically pure thioacetic compound and application thereof to medicine. The optically pure thioacetic compound comprises levorotatory 2-(5-bromo-4-(4-cyclopropyl-naphthalene-1-base)-4H-1,2,4-triazole-3-based sulfenyl) acetic acid and dextral 2-(5-bromo-4-(4-cyclopropyl-naphthalene-1-base)-4H-1,2,4-triazole-3-based sulfenyl) acetic acid.
- -
-
-
- THIO-1,2,4-TRIAZOLE DERIVATIVES AND METHOD FOR PREPARING THE SAME
-
Provided is a process for preparing a compound shown as formula (I), comprising a step of contacting a compound shown as formula (II) or a salt thereof with a brominating agent, wherein R1is OR2 or NR3R4; R2 is C1-C6 alkyl or phenyl; each R3, R4 is independently H, C1-C6 alkyl or cycloalkyl, wherein C1-C6 alkyl, cycloalkyl, or phenyl is optionally further substituted by F, Cl, Br, CH3 or CF3. A process for preparing a compound shown as formula (II), a process for preparing a compound shown as formula (V), a process for preparing a compound shown as formula (III), and an intermediate compound as shown as formula (IIa) or formula (Ib) are also provided.
- -
-
-
- MANUFACTURE OF 2- (5- BROMO-4 (-CYCLOPROPYLNAPHTHALEN-1-YL) -4H-1,2,4-TRIAZOL-3-YLTHIO) ACETIC ACID
-
Described herein are certain processes for the synthesis of compounds of Formula (I):
- -
-
-