207564-70-3

Basic information

• Product Name: tert-butyl (1R,3r,5S)-3-(benzylamino)-8-azabicyclo[3.2.1]octane-8-carboxylate
• Synonyms: tert-butyl (1R,3r,5S)-3-(benzylamino)-8-azabicyclo[3.2.1]octane-8-carboxylate
• CAS NO: 207564-70-3
• Molecular Weight: 316.444
• Mol File: 207564-70-3.mol
• Article Data: 5

Chemical Properties

• CAS DataBase Reference: tert-butyl (1R,3r,5S)-3-(benzylamino)-8-azabicyclo[3.2.1]octane-8-carboxylate(CAS DataBase Reference)
• NIST Chemistry Reference: tert-butyl (1R,3r,5S)-3-(benzylamino)-8-azabicyclo[3.2.1]octane-8-carboxylate(207564-70-3)
• EPA Substance Registry System: tert-butyl (1R,3r,5S)-3-(benzylamino)-8-azabicyclo[3.2.1]octane-8-carboxylate(207564-70-3)

Safety Data

• Hazardous Substances Data: 207564-70-3(Hazardous Substances Data)

Upstream product

• 28957-72-4 N-benzylnortropinone 
• 24424-99-5 di-tert-butyl dicarbonate 
• 542-05-2 acetonedicarboxylic acid 
• 185099-67-6 N-Boc-nortropinone 
• 100-46-9 benzylamine 
• 185099-67-6 Boc-tropinone 

Relevant articles and documents

An imidazopiperidine series of CCR5 antagonists for the treatment of HIV: The discovery of N -{(1 S)-1-(3-fluorophenyl)-3-[(3- endo)-3-(5-isobutyryl-2- methyl-4,5,6,7-tetrahydro-1 H -imidazo[4,5- c ]pyridin-1-yl)-8-azabicyclo[3.2.1] oct-8-yl]propyl}acetamide (PF-232798)

Preventing entry of HIV into human host cells has emerged as an attractive approach to controlling viral replication. Maraviroc 1 is an approved antagonist of the human CCR5 receptor which prevents the entry of HIV. Herein, we report the design and discovery of a series of imidazopiperidine CCR5 antagonists which retain the attractive antiviral profile and window over hERG activity of maraviroc 1, combined with improved absorption profiles in rat and dog. Furthermore, this series of compounds has been shown to retain activity against a laboratory generated maraviroc-resistant HIV-1 strain, which indicates an alternative resistance profile to that of maraviroc 1. Compound 41f (PF-232798) was selected as a clinical candidate from the imidazopiperidine series and is currently in phase II clinical trials.

PIPERAZINO DERIVATIVES AS NEUROKININ ANTAGONISTS

The invention relates to compounds of formula (I) wherein Z, Rc, y, m, u, Ar2, n, X, Rc', l and Ar2 are as described herein. These compounds are neurokinin antagonists. These compounds are useful in the treatment of chronic airway diseases such as asthma.

Tropane derivatives useful in therapy

The present invention provides compounds of formula (I) wherein X, Y, R1, R2 and R3 are as defined hereinabove. The compounds of the present invention are modulators, especially antagonists, of the activity of chemokine CCR5 receptors. Modulators of the CCR5 receptor may be useful in the treatment of various inflammatory diseases and conditions, and in the treatment of infection by HIV and genetically related retroviruses.