1260612-08-5

Basic information

• Product Name: tert-butyl (3R,4R)-4-aMino-3-fluoropiperidine-1-carboxylate
• Synonyms: tert-butyl (3R,4R)-4-aMino-3-fluoropiperidine-1-carboxylate;(3R,4R)-4-AMino-1-Boc-3-fluoropiperidine;Trans-(3R,4R)-1-Boc-4-amino-3-fluoropiperidine;EOS-61545
• CAS NO: 1260612-08-5
• Molecular Formula: C₁₀H₁₉FN₂O₂
• Molecular Weight: 218.27
• Mol File: 1260612-08-5.mol
• Article Data: 4

Chemical Properties

• Boiling Point: 285.6±40.0 °C(Predicted)
• Appearance: /
• Density: 1.11±0.1 g/cm3(Predicted)
• Storage Temp.: 2-8°C(protect from light)
• PKA: 8.88±0.40(Predicted)
• CAS DataBase Reference: tert-butyl (3R,4R)-4-aMino-3-fluoropiperidine-1-carboxylate(CAS DataBase Reference)
• NIST Chemistry Reference: tert-butyl (3R,4R)-4-aMino-3-fluoropiperidine-1-carboxylate(1260612-08-5)
• EPA Substance Registry System: tert-butyl (3R,4R)-4-aMino-3-fluoropiperidine-1-carboxylate(1260612-08-5)

Safety Data

• Hazardous Substances Data: 1260612-08-5(Hazardous Substances Data)

Usage

General Description

Tert-butyl (3R,4R)-4-amino-3-fluoropiperidine-1-carboxylate is a chemical compound with the molecular formula C11H20FN3O2. It is a fluorinated piperidine derivative and is commonly used as a building block in the synthesis of pharmaceutical drugs and other organic compounds. The tert-butyl group attached to the nitrogen atom provides stability and sterically hinders interactions, making the compound useful in drug development. The presence of an amino group and a fluorine atom makes it potentially useful for medicinal chemistry applications, as these functional groups are often found in bioactive compounds. Overall, tert-butyl (3R,4R)-4-amino-3-fluoropiperidine-1-carboxylate is an important intermediate for the synthesis of various pharmaceuticals and organic molecules.

Upstream product

• 211108-50-8 tert-butyl-3-fluoro-4-oxopiperidine-1-carboxylate 
• 211108-48-4 tert-butyl 4-[(trimethylsilyl)oxy]-3,6-dihydropyridine-1(2H)-carboxylate 
• 934536-10-4 (trans)-tert-butyl 4-amino-3-fluoropiperidine-1-carboxylate 
• 79099-07-3 N-tert-butyloxycarbonylpiperidin-4-one 
• 211108-52-0 (3R,4R)-tert-butyl 4-(benzylamino)-3-fluoropiperidine-1-carboxylate 
• 934536-09-1 tert-butyl 4-(benzylamino)-3-fluoropiperidine-1-carboxylate 
• 1070896-84-2 tert-butyl 3-fluoro-4-((methylsulfonyl)oxy)piperidine-1-carboxylate 
• 373604-28-5 3-fluoro-4-hydroxypiperidine-1-carboxylic acid tert-butyl ester 

Relevant articles and documents

Synthesis of a CGRP Receptor Antagonist via an Asymmetric Synthesis of 3-Fluoro-4-aminopiperidine

A practical and efficient enantioselective synthesis of the calcitonin gene-related peptide receptor antagonist 1 has been developed. The key structural component of the active pharmaceutical ingredient is a syn-1,2-amino-fluoropiperidine 4. Two approaches were developed to synthesize this important pharmacophore. Initially, Ru-catalyzed asymmetric hydrogenation of fluoride-substituted enamide 8 enabled the synthesis of sufficient quantities of compound 1 to support early preclinical studies. Subsequently, a novel, cost-effective route to this intermediate was developed utilizing a dynamic kinetic asymmetric transamination of ketone 9. This synthesis also features a robust Ullmann coupling to install a bis-aryl ether using a soluble Cu(I) catalyst. Finally, an enzymatic desymmetrization of meso-diester 7 was exploited for the construction of the γ-lactam moiety in 1.

COMPOUNDS AND COMPOSITIONS AS INHIBITORS OF MEK

The present invention relates to compounds of formula I in which n, R1, R2, R3a, R4 and R5 are defined in the Summary of the Invention; capable of inhibiting the activity of MEK. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of hyperproliferative diseases like cancer.