65057-28-5

Upstream product

• 18650-39-0 (S)-methyl pipecolinate hydrochloride 
• 3105-95-1 pipecolinic acid 
• 26250-84-0 (S)-(-)-1-(tert-butoxycarbonyl)-2-piperidinecarboxylic acid 
• 78058-41-0 (S)-2-carbamoyl-piperidine-1-carboxylic acid tert-butyl ester 
• 741633-48-7 (S)-Piperidine-2-carbonyl chloride 
• 35677-83-9 methyl (S)-pipecolinate 
• 18650-38-9 (R)-piperidine-2-carboxylic acid methyl ester hydrochloride 
• 78058-39-6 (R)-2-Carbamoyl-piperidine-1-carboxylic acid benzyl ester 
• 35677-83-9 (+)-2R-Piperidine-2-carboxylic acid methyl ester 
• 19889-77-1 (RS)-piperidine-2-carboxamide 
• 1723-00-8 (R)-(+)-pipecolic acid 
• 28697-07-6 (R)-1-((benzyloxy)carbonyl)piperidine-2-carboxylic acid 
• 929897-99-4 (2R,1'R)-1-(1'-phenylethyl)piperidine-2-carboxamide 
• 929897-94-9 (2R,1'R)-6-hydroxy-2-(1'-phenylethylamino)hexanenitrile 

Downstream Products

• 189069-80-5 (S)-N-benzyl-piperidine-2-carboxamide 
• 1006872-57-6 (S)-1-(3-(N-(4-(3-phenylisoxazol-5-yl)thiazol-2-yl)thiophene-2-carboxamido)propyl)piperidine-2-carboxamide 
• 1191446-35-1 (2S,αS)-α-(2-carbamoylpiperidinyl)-α-phenylacetic acid methyl ester 
• 1191446-33-9 (2S,αR)-α-(2-carbamoylpiperidinyl)-α-phenylacetic acid methyl ester 
• 1191446-36-2 (4S,9aS)-4-phenylperhydropyrido[1,2-a]pyrazine-1,3-dione 
• 1191446-34-0 (4R,9aS)-4-phenylperhydropyrido[1,2-a]pyrazine-1,3-dione 
• 1358163-34-4 (4S,9aS)-2-benzyl-4-phenylperhydropyrido[1,2-a]pyrazine-1,3-dione 
• 1358013-53-2 (4S,9aS)-2-benzyl-4-phenylperhydropyrido[1,2-a]pyrazine-1,3-dione hydrochloride 
• 1358013-69-0 (4R,9aS)-2-(2-phenylethyl)-4-phenylperhydropyrido[1,2-a]pyrazine-1,3-dione 
• 1358013-57-6 (4S,9aS)-2-(2-phenylethyl)-4-phenylperhydropyrido[1,2-a]pyrazine-1,3-dione 
• 1358013-60-1 ethyl(4S,9aS)-α-(1,3-dioxo-4-phenylperhydropyrido[1,2-a]pyrazin-2-yl)acetate 
• 1374770-27-0 C₁₅H₁₇N₃O₂ 
• 111478-74-1 (R)-2-(aminomethyl)piperidine 
• 1191446-39-5 (2R,αR)-α-(2-carbamoylpiperidinyl)-α-phenylacetic acid methyl ester 

Relevant academic research and scientific papers

Characterization of an enantioselective amidase from Cupriavidus sp. KNK-J915 (FERM BP-10739) useful for enzymatic resolution of racemic 3-piperidinecarboxamide

A novel amidase (CsAM) acting on (R,S)-N-benzyl-3-piperidinecarboxamide was purified from Cupriavidus sp. KNK-J915 (FERM BP-10739) and characterized. The enzyme acts on (R,S)-N-benzyl-3-piperidinecarboxamide S-selectively to yield (R)-N-benzyl-3-piperidinecarboxamide. Analytical gel filtration column chromatography and SDS-PAGE revealed that the enzyme is a tetramer with a subunit of approximately 47 kDa. It has a broad substrate spectrum against nitrogen-containing heterocyclic amides. Its optimal pH and temperature are 8.0-9.0 and 50 °C, respectively. The CsAM gene was cloned and sequenced, and it was found to comprise 1341 bp and encode a polypeptide of 46,388 Da. The deduced amino acid sequence exhibited 78% identity to that of a putative amidase (CnAM) from Cupriavidus necator JMP134. The cultured cells of recombinant Escherichia coli producing CnAM could be used for the S-selective hydrolysis of (R,S)-N-benzyl-3-piperidinecarboxamide but could not be used for the S-selective hydrolysis of (R,S)-3-piperidinecarboxamide because of its very low level of selectivity. In contrast, the cultured cells of recombinant E. coli producing CsAM could hydrolyze both (R,S)-N-benzyl-3-piperidinecarboxamide and (R,S)-3-piperidinecarboxamide with high S-selectivity.

Semi-rigid (Aminomethyl) piperidine-based pentadentate ligands for Mn(II) complexation

Two pentadentate ligands built on the 2-aminomethylpiperidine structure and bearing two tertiary amino and three oxygen donors (three carboxylates in the case of AMPTA and two carboxylates and one phenolate for AMPDA-HB) were developed for Mn(II) complexation. Equilibrium studies on the ligands and the Mn(II) complexes were carried out using pH potentiometry,1H-NMR spectroscopy and UV-vis spectrophotometry. The Mn complexes that were formed by the two ligands were more stable than the Mn complexes of other pentadentate ligands but with a lower pMn than Mn(EDTA) and Mn(CDTA) (pMn for Mn(AMPTA) = 7.89 and for Mn(AMPDA-HB) = 7.07).1H and17O-NMR relaxometric studies showed that the two Mn-complexes were q = 1 with a relaxivity value of 3.3 mM?1 s?1 for Mn(AMPTA) and 3.4 mM?1 s?1 for Mn(AMPDA-HB) at 20 MHz and 298 K. Finally, the geometries of the two complexes were optimized at the DFT level, finding an octahedral coordination environment around the Mn2+ ion, and MD simulations were performed to monitor the distance between the Mn2+ ion and the oxygen of the coordinated water molecule to estimate its residence time, which was in good agreement with that determined using the17O NMR data.

Synthesis and anticonvulsant activity of novel 2,6-diketopiperazine derivatives. Part 2: Perhydropyrido[1,2-a]pyrazines

A new series of chiral pyrido[1,2-a]pyrazine derivatives was synthesised and evaluated in in vivo animal models of epilepsy. A significant influence of the stereochemistry of the pyrido[1,2-a]pyrazine framework on the pharmacological activity was observed

The synthesis and conformational analysis of optical isomers of 4-phenyl-perhydropyrido[1,2-a]pyrazine-1,3-dione: an example of 'solid state-frozen' dynamics in nitrogen-bridged bicyclic 2,6-diketopiperazines

The synthesis, chemical properties, and conformational analysis of enantiopure (4R,9aS)-, (4S,9aR)-, (4S,9aS)-, and (4R,9aR)-4-phenyl-perhydropyrido[1,2-a]pyrazine-1,3-diones having potential biological activity are described. An interesting example of the coexistence of two invertomers of the (4R,9aR)-diastereomer in a single crystal unit cell is reported. The invertomers differ in the cis/trans-relationship between the fused rings and in the absolute configuration at the chiral nitrogen atom. The structure and equilibrium distributions of the respective conformers have been determined by NMR spectroscopy in both polar and non-polar solvents at various temperatures. The NMR spectra show that dynamic processes in the imide parts of the interconverting species are restrained by self-aggregation. The (4S,9aR)-diastereomer exists in a single conformation with insignificant dynamic effects.

An efficient synthesis of enantiomerically pure (R)-pipecolic acid, (S)-proline, and their N-alkylated derivatives

Enantiomerically pure (R)-(+)-pipecolic acid was synthesized in four steps and 42% overall yield starting from dihydropyran and (R)-α- methylbenzylamine. A general short strategy is also described for preparing (S)-proline (47.5% overall yield) and derivatives.

Vanilloid receptor ligands and their use in treatments

Substituted pyridines and pyrimidines and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.

QUINAZOLINE DERIVATIVES

The invention concerns quinazoline derivatives of Formula (I) wherein each of R1, R3, R20, X1, X2, Z, W, (a) and (q) have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of turnours which are sensitive to inhibition of erbB receptor tyrosine kinases, particularly EGFR tyrosine kinase.

Design, Synthesis, and SAR of Potent and Selective Dipeptide-Derived Inhibitors for Dipeptidyl Peptidases

In this paper we report the systematic search for new, potent, and selective DPP II inhibitors. A study of the structure-activity relationship was conducted starting from aminoacyl pyrrolidides as lead compounds. Rational exploration of the P1

ANTITHROMBOTIC AGENTS

Compounds of formula (I): Are antithrombotic agents, having utility in a variety of therapeutic areas including the prevention and/or treatment of deep vein thrombosis (DVT) after surgery, major medical illness, paralysis, malignancy, prolonged immobilisa

Antithrombotic agents

Compounds of formula (I) : are antithrombotic agents, having utility in a variety of therapeutic areas including the prevention and/or treatment of deep vein thrombosis (DVT) after surgery, major medical illness, paralysis, malignancy, prolonged immobilis