3 results about "Rasagiline" patented technology

The present application relates to the preparation method of 2,3-dihydro-1H-inden-1-amine (I) which is an intermediate of anti-Parkinson drug rasagiline and high-risk myelodysplastic syndrome drug pevonedishe, and the preparation reaction is as follows: in a divided electrolytic cell, the cathode electrolyte is composed of the alkaline solution of 2,3-dihydro-1H-inden-1-ketoxime (A) and an organic solvent; the anode electrolyte is an alkaline solution; the cathode electrolysis product of 2,3-dihydro-1H-inden-1-amine (I) is obtained through the electro-reduction reaction.

The invention relates to the technical field of pharmaceutical preparations, and particularly discloses rasagiline pamoate long-acting sustained-release microspheres and a preparation method thereof, the long-acting sustained-release microspheres comprise rasagiline pamoate and a polylactic acid polymer, and the long-acting sustained-release microspheres have a good sustained-release effect. The preparation method comprises the following steps: firstly, preparing rasagiline into pamoate so as to reduce the solubility of rasagiline; in the preparation process of the long-acting sustained-release microspheres, the drug release rate is regulated and controlled by adjusting the proportion of the low-molecular-weight polylactic acid, the sudden drug release phenomenon is reduced by reducing the curing temperature, and the preparation process is suitable for industrial large-scale production. The finally obtained long-acting sustained-release microsphere composition can be used for preparing a medicine for treating Parkinson's disease.

The present application provides a thermostable reductive aminase, its preparation method and application. Specifically, the present application relates to a thermostable reductive aminase and its functional identification and in vitro directed evolution. The reductive aminase of the present application is a reductive aminase from bacteria (BaRedAm) and its mutants (including a reductive aminase mutant with significantly improved enantiomeric selectivity of product rasagiline). The present application also provides an in vitro reductive amination method, comprising the steps of: (i) in the presence of a thermostable reductive aminase BaRedAm, subjecting (S1) a ketone substrate or an aldehyde substrate to a reductive amination reaction with (S2) an amine substrate. The enzyme and mutant of the present application can be used for in vitro enzymatic synthesis of different products such as enantiomerically pure rasagiline.