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

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

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

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.

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

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