22875-63-4

Upstream product

• 675-20-7 piperidin-2-one 
• 105-36-2 ethyl bromoacetate 
• 22041-19-6 ethyl 2-(pyrrolidin-1-yl) acetate 
• 201230-82-2 carbon monoxide 
• 132353-41-4 2-(4'-Bromobutyl)-5-ethoxyoxazole 
• 5414-21-1 5-bromopentan-1-nitrile 

Downstream Products

• 67088-92-0 ethyl-2-(2,4-dichlorophenylhydrazono)-1-piperidineacetate 
• 223254-30-6 1-{4-hydroxy-5-[4-(2-isopropoxy-phenyl)-piperazin-1-yl]-2-oxo-pentyl}-piperidin-2-one 
• 223253-54-1 1-[4-(2-isopropoxy-phenyl)-piperazin-1-yl]-5-(2-oxo-piperidin-1-yl)-pentane-2,4-dione 

Relevant academic research and scientific papers

Silica gel and microwave-promoted synthesis of dihydropyrrolizines and tetrahydroindolizines from enaminones

A wide range of N-(ethoxycarbonylmethyl)enaminones, prepared by the Eschenmoser sulfide contraction between N-(ethoxycarbonylmethyl) pyrrolidine-2-thione and various bromomethyl aryl and heteroaryl ketones, underwent cyclization in the presence of silica gel to give ethyl 6-(hetero)aryl-2,3-dihydro-1H-pyrrolizine-5-carboxylates within minutes upon microwave heating in xylene at 150 °C. Instead of functioning as a nucleophile, the enaminone acted as an electrophile at its carbonyl group during the cyclization. Yields of the bicyclic products were generally above 75%. The analogous microwave-assisted reaction to produce ethyl 2-aryl- 5,6,7,8-tetrahydroindolizine-3-carboxylates from (E)-ethyl 2-[2-(2-oxo-2-arylethylidene)piperidin-1-yl]acetates failed in nonpolar solvents, but occurred in ethanol at lower temperature and microwave power, although requiring much longer time. A possible mechanism for the cyclization is presented, and further functionalization of the newly created pyrrole ring in the dihydropyrrolizine core is described.

Novel solid salt forms of N-[2-[4-[2-(1- methylethoxy)phenyl]-1-piperazinyl]-2-oxo-1piperidineacetamide

The present invention relates to novel solid salt forms of N-[2-[4-[2-(1-methylethoxy)phenyl]-1-piperazinyl]ethyl]-2-oxo-1-piperidineacetamide and processes for their preparation.

Novel heterocycles as selective α1-adrenergic receptor antagonists

A novel series of aryl piperazine substituted heterocycles has been synthesized and identified as antagonists of the α(1a)-adrenergic receptor (α(1a)-AR), which has been implicated in benign prostatic hyperplasia (BPH). These compounds selectively inhibit binding to the α(1a)-AR with K(i)s as low as 2.1 nM. (C) 2000 Elsevier Science Ltd.

Novel arylpiperazines as selective α1-adrenergic receptor antagonists

A novel series of arylpiperazines has been synthesized and identified as antagonists of α(1a) adrenergic receptor (α(1a)-AR) implicated in benign prostatic hyperplasia. These compounds selectively bind to membrane bound α(1a)-AR with K(i)s as low as 0.66 nM. As such, these potentially represent a viable treatment for BPH without the side effects associated with known α1-adrenergic antagonists. (C) 2000 Elsevier Science Ltd. All rights reserved.

Fibrinogen receptor antagonists

Fibrinogen receptor antagonists having the structure, for example, of STR1 for example STR2

A highly efficient synthesis of fibrinogen receptor antagonist L-734,217 via a novel chemoselective silyl-mediated conjugate addition of δ-lactams to 4-vinylpyridine

A highly practical chromatography-free six-step synthesis of L-734,217 suitable for large scale preparation is described. The key chiral pyridine acid intermediate (R)-1 was prepared in four steps based on a novel chemoselective silyl-mediated conjugate a

Process for peptide segment condensation

The present invention is drawn to a process for forming an amide bond linkage comprising reacting a carboxylic acid and an amine in a two-phase mixture of water and an organic solvent selected from an oxygenated organic solvent or an aromatic solvent in the presence of a coupling reagent and an additive. This process is useful for making ubiquitous amides and polypeptides having various biological activities.

Multipath Reactions between Intramolecularly Formed Oxazolium Salts and Nucleophiles

Reaction of 2-(4'-bromobutyl-5-ethoxyoxazole (1) with nucleophiles led either to SN2 substitution products or to products with a piperidine skeleton.The latter were shown to arise from an intramolecular ring closure to an oxazolium salt 7, whic