- Synthesis of 3H, 13C,2H3,15N and 14C-labelled SCH 466036, a histamine 3 receptor antagonist
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The synthesis of [3H]SCH 466036, [Me-3H3]SCH 466036, [13C,2H3,15N]SCH 466036 and [14C]SCH 466036 is described. [3H]SCH 466036 was prepared in two steps via Raney Ni-catalysed exchange with tritiated water. [Me-3H3]SCH 466036 was prepared in a single step from [3H]methyl iodide in 45% yield. [13C,2H3,15N]SCH 466036 was prepared in two steps from [15N] hydroxylamine and [13C,2H3]methyl iodide with an overall yield of 16%. [14C]SCH 466036 was prepared in seven steps from [14C]potassium cyanide in an overall yield of 13%.
- Hesk, David,Borges,Dumpit,Hendershot,Koharski,Lavey,McNamara,Voronin
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- PROCESS FOR PREPARATION OF LASMIDITAN
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The present invention relates to a process for the preparation of lasmiditan, a compound of formula I, or pharmaceutically acceptable salts thereof, the process comprising reacting a compound of formula IX with N-methoxymethylamine or salt thereof to obtain a compound of formula VII; reacting the compound of formula VII with a compound of formula XIV to obtain lasmiditan or salts thereof.
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Paragraph 0186
(2020/06/01)
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- Process method for synthesizing N-substituted piperidine-4-boric acid
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The invention relates to an organic compound synthesis method, and relates to a process method for synthesizing N-substituted piperidine-4-boric acid, which comprises the following steps of: reactingN-substituted piperidine-4-alcohol used as a raw material with thionyl chloride and organic alkali in a solvent to generate N-substituted piperidine-4-chlorine, reacting the N-substituted piperidine-4-chlorine used as a raw material with lithium metal and bis (N, N-dimethylamino) borane halide in a solvent, quenching and acidifying to obtain N-substituted piperidine-4-boric acid. The process method has the advantages of originality, low cost, safety and mild reaction conditions, avoids the dangerous reaction that other patented methods adopt expensive palladium hydroxide hydrogenation, has potential cost advantage and safety advantage, and is suitable for industrial scale-up production.
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Paragraph 0027
(2020/06/17)
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- TRICYCLIC DELTA OPIOID MODULATORS
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The invention is directed to delta opioid receptor modulators. More specifically, the invention relates to tricyclic δ-opioid modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.
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- DIHYDROBENZOTHIOPHENES
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The invention relates to compounds of formula (I), in which W, R1, R2, R3, R4, and q are defined as cited in claim 1. One application for said compounds is the treatment of tumours.
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Page/Page column 78-79
(2010/02/14)
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- Piperidine derivatives for treating psychoses
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The present invention relates to certain novel piperidine derivatives, to processes for their preparation, to pharmaceutical formulations containing them and to their use in medical therapy, particularly in the treatment of psychotic disorders.
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- IMIDAZOYLALKYL SUBSTITUTED WITH A SIX MEMBERED NITROGEN CONTAINING HETEROCYCLIC RING
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Disclosed is a compound of Formula 1.0: STR1 or a pharmaceutically acceptable salt or solvate thereof. Also disclosed are pharmaceutical compositions comprising a pharmaceutically acceptable carrier and an effective amount of a Compound of Formula 1.0. Further disclosed is a method of treating allergy (for example asthma), inflammation, hypertension, raised intraocular pressure (such as glaucoma)--i.e., a method of lowering intraocular pressure, sleeping disorders, states of hyper and hypo motility and acidic secretion of the gastrointestinal tract, hypo and hyperactivity of the central nervous system (for example, agitation and depression) and other CNS disorders (such as Alzheimers, Schizophrenia, and migraine) comprising administering an effective amount of a compound of Formula 1.0 to a patient in need of such treatment.
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- Imidazoylalkyl substituted with a six membered nitrogen containing heterocyclic ring
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Disclosed is a compound of Formula 1.0: STR1 or a pharmaceutically acceptable salt or solvate thereof. Also disclosed are pharmaceutical compositions comprising a pharmaceutically acceptable carrier and an effective amount of a Compound of Formula 1.0. Further disclosed is a method of treating allergy (for example asthma), inflammation, hypertension, raised intraocular pressure (such as glaucoma)--i.e., a method of lowering intraocular pressure, sleeping disorders, states of hyper and hypo motility and acidic secretion of the gastrointestinal tract, hypo and hyperactivity of the central nervous system (for example, agitation and depression) and other CNS disorders (such as Alzheimers, Schizophrenia, and migraine) comprising administering an effective amount of a compound of Formula 1.0 to a patient in need of such treatment.
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