1919868-77-1

Basic information

• Product Name: (R)-2-(2,5-difluorophenyl)pyrrolidine (R)-2-hydroxysuccinate
• Synonyms: (R)-2-(2,5-difluorophenyl)pyrrolidine (R)-2-hydroxysuccinate;(R)-2-(2,5-Difluorophenyl)pyrrolidine Malic acid
• CAS NO: 1919868-77-1
• Molecular Formula: C14H17F2NO5
• Molecular Weight: 317.29
• Mol File: 1919868-77-1.mol
• Article Data: 10

Chemical Properties

• Appearance: /
• Density: 1.389 at 20℃
• Vapor Pressure: 0.005Pa at 20℃
• CAS DataBase Reference: (R)-2-(2,5-difluorophenyl)pyrrolidine (R)-2-hydroxysuccinate(CAS DataBase Reference)
• NIST Chemistry Reference: (R)-2-(2,5-difluorophenyl)pyrrolidine (R)-2-hydroxysuccinate(1919868-77-1)
• EPA Substance Registry System: (R)-2-(2,5-difluorophenyl)pyrrolidine (R)-2-hydroxysuccinate(1919868-77-1)

Safety Data

• Hazardous Substances Data: 1919868-77-1(Hazardous Substances Data)

Usage

General Description

The chemical (R)-2-(2,5-difluorophenyl)pyrrolidine (R)-2-hydroxysuccinate is a compound with a molecular structure that includes a pyrrolidine ring, a difluorophenyl group, and a hydroxysuccinate moiety. (R)-2-(2,5-difluorophenyl)pyrrolidine (R)-2-hydroxysuccinate is classified as a pyrrolidine derivative and can be used in organic synthesis and medicinal chemistry. It may have potential applications in pharmaceuticals and agrochemicals due to its unique structure and properties. The (R)-2-hydroxysuccinate group may also have implications for chiral catalysis and asymmetric synthesis. Further research and development of this compound could lead to its incorporation into various processes and products in the chemical industry.

Upstream product

• 636-61-3 D-Malic acid 
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• 886503-15-7 rac-2-(2,5-difluorophenyl)pyrrolidine 
• 1216260-42-2 4‐chloro‐1‐(2,5-difluorophenyl)butan-1-one 
• 2646-90-4 2,5-difluorobenzaldehyde 
• 399-94-0 2-bromo-1,4-difluorobenzene 

Downstream Products

• 2135871-21-3 phenyl (5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-3,3a-dihydropyrazolo[1,5-a]pyrimidin-3-yl)carbamate 
• 1223404-88-3 5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidin-3-amine 
• 1223405-08-0 (S)-N-(5-((R)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate 
• 1218935-59-1 (R)-(+)-2-(2,5-difluorophenyl)pyrrolidine 

Relevant articles and documents

Racemization method of larotinib intermediate

The invention discloses a racemization method of a larotinib intermediate, which comprises the following steps: in a solvent, heating (2S)-2-(2, 5-difluorophenyl)pyrrolidine(compound I, S-type I) or aracemic mixture mainly comprising S-type I, and convert

Synthesis method of (R)-2-(2, 5-difluorophenyl) pyrrolidine

The invention belongs to the technical field of chemical pharmacy, and relates to a synthetic method of (R)-2-(2, 5-difluorophenyl)pyrrolidine. The synthesis method comprises the following steps: (1) carrying out dehydration condensation reaction on a compound as shown in a formula 1 and a chiral induction reagent (R) tert-butylsulfinamide to obtain a compound as shown in a formula 2; (2) carrying out addition reaction on the compound in the formula 2 and a Grignard reagent to obtain a compound in a formula 3; (3) carrying out a reduction/cyclization reaction on the compound shown in the formula 3, trifluoroacetic acid and triethylsilane to obtain a compound shown in a formula 4; (4) splitting the compound shown in the formula 4 by (D)-malic acid to obtain the (R)-2-(2, 5-difluorophenyl) pyrrolidine*D malate compound with EE being greater than 98% shown in the formula 5; and (5) dissociating the compound in the formula 5 with a sodium hydroxide solution to obtain (R)-2-(2, 5-difluorophenyl) pyrrolidine. By utilizing the synthetic method of (R)-2-(2,5-difluorophenyl)pyrrolidine, the cost is low, the optical purity is high, the subsequent separation process is simplified, the raw materials are easy to obtain, the process conditions are mild, and the synthetic method is suitable for synthesizing (R)-2-(2, 5-difluorophenyl) pyrrolidine in large-scale production.

Method for preparing larotrectinib intermediate through one-pot method

The invention discloses a method for preparing a larotrectinib intermediate through a one-pot method. The preparation method is characterized by comprising the following steps: 1) dissolving a compound VI serving as a raw material in a solvent, adding isopropyl magnesium chloride to generate a Grignard reagent, and reacting with N-Boc-pyrrolidone to obtain a compound I; 2) adding an acid into thereaction solution, and carrying out a Boc removal reaction on the compound I to obtain a compound II; 3) adding an alkali into the reaction solution, and carrying out a ring closing reaction on the compound II to obtain a compound III; 4) carrying out reduction on the compound III in the reaction solution to obtain a compound IV; and 5) carrying out salification on the compound IV and D-malic acid, and re-crystallizing to obtain a compound V.