69319-32-0

Upstream product

• 60725-36-2 2-[{2-[hydroxyl(phenyl)methyl]benzyl}(methyl)amino]ethanol 
• 24833-47-4 2-benzoyl-N-(2-hydroxyethyl)-N-methylbenzamide 
• 22103-85-1 2-benzoylbenzoyl chloride 
• 85-52-9 2-Benzoylbenzoic acid 
• 17494-19-8 2,3-dihydro-9b-phenyloxazolo<2,3-a>isoindol-5(9bH)-one 
• 23327-57-3 nefopam hydrochloride 
• 18409-76-2 2-(1-phenyl-2,3-dihydro-1H-isoindol-2-yl)ethanol 
• 84940-28-3 1-phenyl-3,4,5,6-tetrahydro-1H-2,5-benzoxazocine-5-carbonitrile 

Downstream Products

• 91463-82-0 (R)-5-methyl-1-phenyl-1,3,4,6-tetrahydro-2,5-benzoxazocine 
• 119-61-9 benzophenone 
• 13831-42-0 2-[(2-benzylbenzyl)(methyl)amino]ethanol 
• 60725-36-2 2-[{2-[hydroxyl(phenyl)methyl]benzyl}(methyl)amino]ethanol 
• 23327-57-3 nefopam hydrochloride 
• 129356-73-6 (+/-)-nefopam methiodide 
• 66091-32-5 (1R,5S)/(1S,5R)-nefopam N-oxide 
• 66091-32-5 (1R,5R)/(1S,5S)-nefopam N-oxide 
• 129356-74-7 Nefopam trideuteriomethioiodide 
• 129356-74-7 Nefopam trideuteriomethioiodide 
• 865-50-9 iodomethane-d3 

Relevant academic research and scientific papers

Old is Gold? Nefopam Hydrochloride, a Non-opioid and Non-steroidal Analgesic Drug and Its Practical One-Pot Synthesis in a Single Solvent for Large-Scale Production

Nefopam hydrochloride is extensively used in most of the European countries until today as an analgesic because of its non-opiate (non-narcotic) and non-steroidal action with fewer side effects compared with opioid and other analgesics, which cause more troublesome side effects. A multikilogram synthesis of nefopam hydrochloride has been achieved in one pot using a single solvent (toluene). A ≥99.9% purity of the active pharmaceutical ingredient (API) was achieved in excellent overall yield (≥79%). The one-pot, five-step synthetic process involves formation of an acid chloride (3) from benzoylbenzoic acid (2) followed by amidation (4), reduction (5), cyclization (6), and formation of the hydrochloride salt (1). The major advantages include (i) use of a single solvent, (ii) >90% conversion in each step, (iii) a cost-effective and operationally friendly process, (iv) averting the formation of genotoxic impurities, and (v) improved overall yield (≥79%) provided by the one-pot operation. For the first time, we report the characterization data of API 1, intermediates 3, 4, and 5, and also a possible impurity (5a).

MALODOR COUNTERACTING COMPOSITION AND AGENT AND THE USE THEREOF

The present invention relates to a malodor counteracting composition. In particular the invention relates to a malodor counteracting composition comprising nefopam, or a polymorph, a hydrate or a solvate thereof. The invention also relates to the use of said composition and attenuator or suppressor, for attenuating or suppressing malodors, in particular earthy, musty and/or moldy malodors.

A PROCESS FOR THE RESOLUTION OF NEFOPAM

A process for increasing the optical purity of a mixture of enantiomers of nefopam uses a substantially single enantiomer of a O,O-diaroyltartaric acid as a resolving agent, via a bisnefopam salt of the acid. This salt is new.

Synthesis of Some 2,5-Benzoxazocine and 2,6-Benzoxazonine Derivatives from ω-(Dihydroisoindol-2-yl)alkanol Precursors by Means of Cyanogen Bromide

Reaction of cyanogen bromide with 2-(1-phenyl-2,3-dihydro-1H-isoindol-2-yl)ethanol (5a) gave 1-phenyl 3,4,5,6-tetrahydro-1H-2,5-benzoxazocine-5-carbonitrile (6a) in a low to moderate yield..Similarly, 3-(1-phenyl-2,3-dihydro-1H-isoindol-2-yl)propan-1-ol (5c) gave 1-phenyl-1,3,4,5,6,7-hexahydro-2,6-benzoxazonine-6-carbonitrile (6c).The analogous 1-(4-methoxyphenyl) derivatives of both medium ring systems were also prepared, and some mechanistic aspects of the results are discussed.Conversion of (6a) into the analgesic, Nefopam, is described.