40432-52-8

Usage

Chemical Properties

White powder

InChI:InChI=1/C16H18N2/c17-15-11-18(12-15)16(13-7-3-1-4-8-13)14-9-5-2-6-10-14/h1-10,15-16H,11-12,17H2

Upstream product

• 143699-92-7 3-Azido-1-benzhydryl-azetidine 
• 91-00-9 Benzhydrylamine 
• 63477-43-0 3-chloro-1-diphenylmethylamino-2-hydroxypropane 
• 33301-41-6 1-benzhydryl-3-azetidinyl methanesulfonate 
• 40320-60-3 N-benzhydryl 3-azetidinone 
• 1375075-83-4 C₁₆H₁₆N₂O*ClH 
• 18621-17-5 1-(diphenylmethyl)-3-hydroxyazetidine 
• 91189-18-3 tert-butyl (1-benzhydrylazetidin-3-yl)carbamate 
• 38353-74-1 2-(1-benzhydrylazetidin-3-yl)isoindoline-1,3-dione 

Downstream Products

• 510729-14-3 (1-benzhydryl-azetidin-3-yl)-(2-fluoro-4-nitro-phenyl)-amine 
• 817555-03-6 N-[1-(diphenylmethyl)-3-azetidinyl]methanesulfonamide 
• 91189-18-3 tert-butyl (1-benzhydrylazetidin-3-yl)carbamate 
• 256526-41-7 (2S)-N₂-(1-diphenylmethyl-3-azetidinyl)-1-(1,3-benzoxazol-2-yl)-2-piperidinecarboxamide 
• 321344-94-9 1-(1-diphenylmethylazetidin-3-yl)-3-(4-fluorophenyl)-2-(pyridin-4-yl)-1H-pyrrole 
• 337511-57-6 1-(diphenylmethyl)-3-[(2-nitrophenylmethyl)amino]-azetidine 
• 893565-91-8 C₅₉H₈₇N₃O₁₅ 
• 942308-13-6 1-benzhydryl-3-(N,N-dicyclopropylamino)-3-azetidine 
• 132920-58-2 ethyl 1-(1-diphenylmethylazetidin-3-yl)-6,7-difluoro-1,4-dihydro-4-oxoquinolin-3-carboxylate 
• 102065-87-2 N-(1-benzhydryl-azetidin-3-yl)-acetamide 

Relevant academic research and scientific papers

Synthesis and biological evaluation of novel azetidine derivatives as dopamine antagonist

In this study, azetidine derivatives were evaluated for their potency as dopaminergic antagonist. The study comprised derivatives substituted in 3-position with amide moiety. Further, the phenyl moiety of amide was modified at 2, 3, or 4-position. The substituted compounds were biologically evaluated for their affinity for D2 and D4 receptors. The most potent D2 and D4 antagonist among these compounds appeared to be the N-(1-benzhydryl-azetidin-3yl)-2-bromo-benzamide and N-(1-benzhydryl-azetidin-3yl)-4-bromo-benzamide, respectively. Various docking interactions of CPPMA with the D4 receptor and the same for compound 5 i.e., N-(1-benzhydryl-azetidin-3yl)-4-bromo-benzamide were found to have good correlation with observed biological activity.

Process development of a novel azetidinyl ketolide antibiotic

Process development and the multikilogram synthesis of a novel azetidinyl ketolide antibiotic is described. Starting with clarithromycin, the eight-step synthesis features several telescoped operations and direct isolations, which results in a significant improvement in throughput and a major reduction in solvent usage and waste stream volume over the first scale-up campaign. Particular highlights of this effort include the development of an efficient synthesis of 3-hydroxy-1,5-naphthyridine-4-carbaldehyde via a Skraup process and engineering a robust final API synthesis. We also discovered a crystalline monotosylate salt that addressed significant formulation and degradation issues experienced when using the noncrystalline freebase.

Arylalkane, arylalkene and aryl azaalkane, medicaments containing said compounds and method for the production thereof

The present invention relates to compounds of general formula [in-line-formulae]R—Z1—Z2—Z3—R1, ??(I)[/in-line-formulae] wherein R, R1 and Z1 to Z3 are defined as in claim 1, the tautomers, the diastereomers, the enantiomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, particularly CGRP-antagonistic properties, pharmaceutical compositions containing these compounds, their use and processes for preparing them.

DIRECT AMINOLYSIS

In some aspects, the present invention provides a method of preparing a compound of the formula (I) comprising reacting a mesylate compound of the formula (II) by direct aminolysis with a reagent comprising ammonia. The reaction is preferably carried out

An efficient two-step synthesis of 3-amino-1-benzhydrylazetidine

A streamlined process for the synthesis of 3-amino-1-benzhydrylazetidine is described. Commercially available 1-benzhydrylazetidin-3-ol was reacted with methanesulfonyl chloride in the presence of triethylamine in acetonitrile, upon quench with water, the

Aqueous phosphoric acid as a mild reagent for deprotection of tert-butyl carbamates, esters, and ethers

(Chemical Equation Presented) Aqueous phosphoric acid (85 wt %) is an effective, environmentally benign reagent for the deprotection of tert-butyl carbamates, tert-butyl esters, and tert-butyl ethers. The reaction conditions are mild and offer good selectivity in the presence of other acid-sensitive groups, including CBZ carbamates, azetidine, benzyl and methyl esters, TBDMS, and methyl phenyl ethers. The mildness of the reaction is further demonstrated in the synthesis of clarithromycin derivative 4, in which a tert-butyl ester is removed in the presence of cyclic carbamate, lactone, ketal, acetate ester, and epimerizable methyl ketone functionalities. The reaction preserves the stereochemical integrity of the substrates. The reactions are high yielding, and the workup is convenient.

PYRAZOLE DERIVATIVE

Not available

N-HETEROCYCLYL-SUBSTITUTED AMINO-THIAZOLE DERIVATIVES AS PROTEIN KINASE INHIBITORS

Aminothiazole compounds with N-containing cycloalkyl at the 2-amino position which are represented by the Formula (I), or a pharmaceutically acceptable prodrug of said compound, or pharmaceutically acceptable salt of said compound, modulate and/or inhibit the cell proliferation and activity of protein kinases.

Thiophene derivatives useful as anticancer agents

The invention relates to compounds of the formula 1 or a pharmaceutically acceptable salt and to pharmaceutically acceptable salts and hydrates thereof, wherein X, Y, R1, R2 and R11 are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating hyperproliferative disorders in a mammal by administering the compounds of formula 1.