1007089-84-0

Basic information

• Product Name: 3-(chloromethyl)-5-methylpyridine hydrochloride
• Synonyms: 3-(chloromethyl)-5-methylpyridine hydrochloride
• CAS NO: 1007089-84-0
• Molecular Formula: C7H9Cl2N
• Molecular Weight: 178.05906
• Mol File: 1007089-84-0.mol

Chemical Properties

• Boiling Point: 232.233 °C at 760 mmHg
• Flash Point: 116.576 °C
• Appearance: /
• Density: 1.118 g/cm³
• Storage Temp.: Refrigerator
• Solubility: DMSO (Slightly), Methanol (Slightly), Water (Slightly)
• CAS DataBase Reference: 3-(chloromethyl)-5-methylpyridine hydrochloride(CAS DataBase Reference)
• NIST Chemistry Reference: 3-(chloromethyl)-5-methylpyridine hydrochloride(1007089-84-0)
• EPA Substance Registry System: 3-(chloromethyl)-5-methylpyridine hydrochloride(1007089-84-0)

Safety Data

• Hazardous Substances Data: 1007089-84-0(Hazardous Substances Data)

Usage

Uses

3-Chloromethyl-5-methylpyridine is an intermediate in the synthesis of Rupatadine (R701650).

Upstream product

• 102074-19-1 (5-methylpyridin-3-yl)methanol 
• 591-22-0 3,5-Lutidine 
• 29681-45-6 5-methylnicotinic acid methyl ester 

Relevant articles and documents

Expedient synthesis of rupatadine

Rupatadine, a new potent, orally active dual antagonist of histamine and platelet-activating factor (PAF), has been synthesized in 91% overall yield. Copyright Taylor & Francis Group, LLC.

Preparation method of rupatadine fumarate intermediate 5-methyl-3-chloromethylpyridine hydrochloride

The present invention relates to a preparation method for a rupatadine fumarate intermediate, namely 5-methyl-3-chloromethylpyridine hydrochloride. The preparation method comprises the following steps: 1, carrying out a reaction on a 5-methyl-3-hydroxymethylpyridine solution and thionyl chloride to generate 5-methyl-3-chloromethylpyridine hydrochloride; and 2, carrying out reduced-pressure concentration to remove a part of a solvent in reaction liquid, adding an organic solvent for rapid crystallization, and conducting stirring and filtering to obtain the 5-methyl-3-chloromethylpyridine hydrochloride.

Preparation process of Rupatadine

The invention discloses a rupatadine preparation process, which comprises: S1, preparing methyl 5-methylnicotinate; S2, preparing 5-methyl-3-pyridinemethanol; S3, preparing 3-methyl-5-chloromethylpyridine hydrochloride; and S4, preparing rupatadine. According to the present invention, the preparation process has advantages of low cost, mild reaction condition, simple operation, low requirement onequipment, good product purity and high yield, and is suitable for large-scale industrial production.

Synthesis method of rupatadine intermediate namely 3-chloromethyl-5-methylpyridine

The invention discloses a synthesis method of a rupatadine intermediate namely 3-chloromethyl-5-methylpyridine. The method comprises the following steps: (1) adding 3,5-dimethylpyridine and concentrated sulfuric acid into a reactor with UV radiation; (2) introducing chlorine gas into the reactor in the step (1), and carrying out reactions for 12 to 24 hours under the irradiation of UV light; (3) adding water into the solution obtained in the step (2) after reactions until the pH value of the solution falls in the weak alkaline area; (4) extracting the solution obtained in the step (3) by toluene, then introducing hydrogen chloride gas into the toluene layer to precipitate the product, and re-crystallizing the obtained product to obtain a pure product of 3-chloromethyl-5-methylpyridine hydrochloride. The provided method can industrially obtain 3-chloromethyl-5-methylpyridine in a low cost.

4H- [1, 2, 4] TRIAZOLO [5, 1 -B] PYRIMIDIN-7 -ONE DERIVATIVES AS CCR2B RECEPTOR ANTAGONISTS

The present invention relates to novel compounds for use in the compositions, to processes for their preparation, to intermediates useful in their preparation and to their use as therapeutic agents. The present invention also relates to pharmaceutical com

Synthesis, in vitro and in vivo activity of thiamine antagonist transketolase inhibitors

Tumor cells extensively utilize the pentose phosphate pathway for the synthesis of ribose. Transketolase is a key enzyme in this pathway and has been suggested as a target for inhibition in the treatment of cancer. In a pharmacodynamic study, nude mice with xenografted HCT-116 tumors were dosed with 1 ('N3′-pyridyl thiamine'; 3-(6-methyl-2-amino-pyridin-3-ylmethyl)-5-(2-hydroxy-ethyl)-4-methyl-thiazol-3-ium chloride hydrochloride), an analog of thiamine, the co-factor of transketolase. Transketolase activity was almost completely suppressed in blood, spleen, and tumor cells, but there was little effect on the activity of the other thiamine-utilizing enzymes α-ketoglutarate dehydrogenase or glucose-6-phosphate dehydrogenase. Synthesis and SAR of transketolase inhibitors is described.