- Synthesis method of 2-amino methyl pyrimidine hydrochloride and derivatives thereof
-
The invention relates to preparation of one medicine intermediate, in particular relates to a preparation method of 2-aminomethylpyrimidine hydrochloride and derivatives thereof. The preparation method is improved by overcoming the defects of an industrial production technology and a laboratory technology which are commonly used at present, improvements are as follows: the method takes 2-cyanopyrimidine and derivatives thereof as starting materials, Boc anhydride is adopted as a protective agent, reduction-protection one-pot reaction is carried out under alkaline condition, and then hydrogen chloride deprotection is carried out, so that the 2-aminomethylpyrimidine hydrochloride and the derivatives thereof are prepared. According to the method provided by the invention, the reaction period is short, the conversion rate is high, the product quality is good, and the content of the produced 2-aminomethylpyrimidine hydrochloride and the derivatives thereof is more than 99%; meanwhile, operation steps are simple, required equipment is simple, and energy consumption is low.
- -
-
Paragraph 0014; 0016; 0018; 0020; 0022
(2017/07/21)
-
- Preparation method of 2-amido methylpyrimidine hydrochloride
-
The invention discloses a preparation method of 2-amido methylpyrimidine hydrochloride, and relates to the technical field of organic synthesis. The preparation method comprises the steps that 2-amido methylpyrimidine mesylate is taken as a raw material, sodium methylate is added at certain temperature, suction filtration is conducted after reacting is finished, the temperature of filtrate is decreased to certain temperature, an enough amount of hydrochloric acid gas is introduced, and stirring and filtering are conducted to obtain the product 2-amido methylpyrimidine hydrochloride. The 2-amido methylpyrimidine hydrochloride is simple in preparation technology, low in cost and simple in aftertreatment; in addition, the product purity reaches 99.5% or above, the yield reaches 85% or above, and the preparation method is suitable for industrialized production.
- -
-
Paragraph 0013; 0014; 0015; 0016; 0017; 0018; 0019; 0020
(2017/06/02)
-
- PROCESS FOR THE PREPARATION OF (S)-4-[(3-CHLORO-4-METHOXYBENZYL)AMINO]-2-[2- (HYDROXYMETHYL)-1-PYRROLIDINYL]-N-(2-PYRIMIDINYL METHYL-5-PYRIMIDINE CARBOXAMIDE
-
The present invention relates to an improved process for the preparation of (S)-4-[(3- chloro-4-methoxybenzyl)amino]-2-[2-(hydroxymethyl)-1-pyrrolidinyl]-N-(2-pyrimidinyl ethyl)- 5-pyrimidine carboxamide compound of formula-1 represented by the following structural formula.
- -
-
Page/Page column 22; 23
(2015/01/16)
-
- SPIRO-LACTAM NMDA RECEPTOR MODULATORS AND USES THEREOF
-
Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
- -
-
Paragraph 0139
(2014/08/19)
-
- AZINYL IMIDAZOAZINE AND AZINYL CARBOXAMIDE
-
Azinyl imidazoazines of formula (I), in which the symbols have the meanings indicated in the description, are disclosed, as well as their salts and N oxides, processes for producing the same and new intermediate products. The use of the compounds of formula I and of the intermediate products for combating animal pests and undesirable micro-organisms is also disclosed.
- -
-
Page/Page column 88-89
(2010/02/14)
-
- Cyclic compounds
-
1. A cyclic compound of the formula (I) or a pharmacologically acceptable salt thereof, wherein X is ═CH— or ═N—, Y is —NH—, —NR4—, —S—, —O—, —CH═N—, —N═CH—, —N═N—, —CH═CH—, etc., R1 is a lower alkoxy group, an amino group, a heterocyclic ring containing N atom(s), or a hydroxy group substituted by a heterocyclic ring containing N atom(s) (each of which is optionally substituted), R2 is a lower alkylamino group which is optionally substituted by an aryl group, a lower alkoxy group which is optionally substituted by an aryl group, a lower alkoxy group substituted by an aromatic heterocyclic ring containing N atom(s), R3 is an aryl group, a heterocyclic ring containing N atom(s), a lower alkyl group, a lower alkoxy group, a cyclo lower alkoxy group, a hydroxy group substituted by a heterocyclic ring containing N atom(s), or an amino group (each of which is optionally substituted), and R3 and a substituent in Y may be combined to form a lactone ring. The compound of the present invention has excellent selective PDE V inhibitory activity and therefore, is useful as a therapeutic or prophylactic drug for treating various diseases due to functional disorders on cGMP-signaling.
- -
-
-