1334320-82-9

Basic information

• Product Name: trans-4-Fluoro-3-hydroxyp...
• Synonyms: trans-4-Fluoro-3-hydroxyp...;trans-4-Fluoro-3-hydroxypyrrolidine hydrochloride;trans-4-Fluoropyrrolidin-3-ol
• CAS NO: 1334320-82-9
• Molecular Formula: C4H9ClFNO
• Molecular Weight: 141.57
• Mol File: 1334320-82-9.mol
• Article Data: 7

Chemical Properties

• Boiling Point: 188.2±40.0 °C(Predicted)
• Appearance: /
• Density: 1.19±0.1 g/cm3(Predicted)
• PKA: 13.71±0.40(Predicted)
• CAS DataBase Reference: trans-4-Fluoro-3-hydroxyp...(CAS DataBase Reference)
• NIST Chemistry Reference: trans-4-Fluoro-3-hydroxyp...(1334320-82-9)
• EPA Substance Registry System: trans-4-Fluoro-3-hydroxyp...(1334320-82-9)

Safety Data

• Hazardous Substances Data: 1334320-82-9(Hazardous Substances Data)

Usage

Description

Trans-4-Fluoro-3-hydroxy-L-proline is a chemical compound that belongs to the family of amino acids. It is a derivative of proline, a nonessential amino acid that plays a crucial role in the structure and function of proteins. The addition of a fluorine atom and a hydroxyl group to the proline structure enhances its potential pharmaceutical and medicinal applications. Trans-4-Fluoro-3-hydroxy-L-proline has been studied for its potential antiviral and antitumor properties, as well as its ability to act as a precursor for the synthesis of novel pharmaceutical compounds. Additionally, its unique chemical structure makes it a valuable tool in research and drug development for various applications in the fields of medicine and biotechnology.

Uses

Used in Pharmaceutical Industry:
Trans-4-Fluoro-3-hydroxy-L-proline is used as a pharmaceutical compound for its potential antiviral and antitumor properties. Its unique chemical structure allows it to be a valuable tool in research and drug development for various applications in the fields of medicine and biotechnology.
Used in Drug Development:
Trans-4-Fluoro-3-hydroxy-L-proline is used as a precursor for the synthesis of novel pharmaceutical compounds. Its unique chemical structure and potential antiviral and antitumor properties make it a promising candidate for the development of new drugs and therapies.

Upstream product

• 1174020-49-5 tert-butyl (cis)-3-fluoro-4-hydroxypyrrolidine-1-carboxylate 
• 1379325-25-3 3-hydroxy-4-fluoro-N-tert-butoxycarbonylpyrrolidine 
• 1523530-25-7 racemic-trans-4-fluoro-3-hydroxypyrrolidine hydrochloride 

Relevant articles and documents

Identification of 4-(Aminomethyl)-6-(trifluoromethyl)-2-(phenoxy)pyridine Derivatives as Potent, Selective, and Orally Efficacious Inhibitors of the Copper-Dependent Amine Oxidase, Lysyl Oxidase-Like 2 (LOXL2)

LOXL2 catalyzes the oxidative deamination of ε-amines of lysine and hydroxylysine residues within collagen and elastin, generating reactive aldehydes (allysine). Condensation with other allysines or lysines drives the formation of inter- and intramolecular cross-linkages, a process critical for the remodeling of the ECM. Dysregulation of this process can lead to fibrosis, and LOXL2 is known to be upregulated in fibrotic tissue. Small-molecules that directly inhibit LOXL2 catalytic activity represent a useful option for the treatment of fibrosis. Herein, we describe optimization of an initial hit 2, resulting in identification of racemic-trans-(3-((4-(aminomethyl)-6-(trifluoromethyl)pyridin-2-yl)oxy)phenyl)(3-fluoro-4-hydroxypyrrolidin-1-yl)methanone 28, a potent irreversible inhibitor of LOXL2 that is highly selective over LOX and other amine oxidases. Oral administration of 28 significantly reduced fibrosis in a 14-day mouse lung bleomycin model. The (R,R)-enantiomer 43 (PAT-1251) was selected as the clinical compound which has progressed into healthy volunteer Phase 1 trials, making it the “first-in-class” small-molecule LOXL2 inhibitor to enter clinical development.

(HETERO)ARYLAMIDE COMPOUND FOR INHIBITING PROTEIN KINASE ACTIVITY

Provided are a (hetero)arylamide compound as shown in formula (I) having an inhibitory effect on protein kinase activity, a pharmaceutically acceptable salt, a stereoisomer, a solvate or hydrate thereof, a pharmaceutical composition comprising the compound or a derivative thereof, and a method for preparing the compound. The compound can be used as an irreversible inhibitor for protein kinase for preparing a plurality of drugs comprising an anti-tumour drug.

CRYSTALLINE FORMS OF A LYSYL OXIDASE-LIKE 2 INHIBITOR AND METHODS OF MAKING

Described herein are crystalline forms of pharmaceutically acceptable salts of the lysyl oxidase-like 2 (LOXL2) inhibitor (3-(4-(aminomethyl)-6-(trifluoromethyl)pyridin-2-yloxy)phenyl)((3R,4R)-3-fluoro-4-hydroxypyrrolidin-1-yl)methanone. Also described are methods of making the LOXL2 inhibitor, pharmaceutical compositions and medicaments comprising the LOXL2 inhibitor, and methods of using the LOXL2 inhibitor in the treatment of conditions, diseases, or disorders associated with LOXL2 activity.