864829-49-2

Upstream product

• 116386-68-6 (S)-4-(1-Methylethyl)-3-(1-oxo-4-pentenyl)-2-oxazolidinone 
• 95791-03-0 (2S)-2-[(benzyloxy)methyl]pent-4-en-1-ol 
• 39716-58-0 pent-4-enoyl chloride 
• 864829-47-0 (2R)-2-[(benzyloxy)methyl]pent-4-enoic acid 
• 864829-46-9 (4S)-3-{(2R)-2-[(benzyloxy)methyl]pent-4-enoyl}-4-isopropyloxazolidin-2-one 
• 3430-17-9 2-bromo-3-picoline 
• 864829-48-1 (2R)-2-[(benzyloxy)methyl]-1-iodopent-4-ene 

Downstream Products

• 864829-50-5 (7R)-7-[(benzyloxy)methyl]-9-methylene-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridine 

Relevant academic research and scientific papers

Practical syntheses of enantiomerically pure key intermediates of opioid receptor-like 1 (ORL1) antagonists

Practical syntheses of enantiomerically pure key intermediates of opioid receptor-like 1 (ORL1) antagonists are described. Our synthetic methodology features the preparation of multigram quantities of seven-membered key intermediate (-)-3 and six-membered one (-)-4 without the use of toxic tin reagents. In the case of (-)-3, the key step involved diastereoselective reduction using a sterically hindered reducing reagent. Our methodology allows for facile scale-up to afford the products in multigram quantities [in the case of (-)-4, >100-g quantities). These convenient approaches facilitate structure-activity relationship studies including in vivo cardiovascular adverse effects. Georg Thieme Verlag Stuttgart.

CYCLOALKANOPYRIDINE DERIVATIVE

Provided are cycloalkanopyridine derivatives of formula [I]: [wherein the symbols are the same as those stated in the description]. The compounds act as a nociceptin receptor antagonist, and are useful as medicines for diseases associated with a nociceptin receptor, for example, as a reliever against tolerance to a narcotic analgesic; a reliever against dependence on or addiction to a narcotic analgesic; an analgesic enhancer; an antiobesitic or appetite suppressor; a treating or prophylactic agent for cognitive impairment and dementia/amnesia; an agent for treating developmental cognitive abnormality; a remedy for schizophrenia; an agent for treating neurodegenerative diseases; an anti-depressant or treating agent for affective disorder; a treating or prophylactic agent for diabetes insipidus; a treating or prophylactic agent for polyuria; or a remedy for hypotension.