Awesome Chemistry Experiments For (R)-tert-Butyl 3-(hydroxymethyl)piperidine-1-carboxylate

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IMIDAZOPYRAZINES AS LSD1 INHIBITORS

The present invention is directed to imidazo[1,2-a]pyrazine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer.

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Piperidine – Wikipedia,
Piperidine | C5H17427N – PubChem

 

New explortion of 2213-43-6

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Reductive alkylation of hydrazine derivatives with alpha-picoline-borane and its applications to the syntheses of useful compounds related to active pharmaceutical ingredients

An efficient method for the direct reductive alkylation of hydrazine derivatives with alpha-picoline-borane has been developed to synthesize a variety of N-alkylhydrazine derivatives. This method provided N,N-dialkylhydrazine derivatives and N-monoalkylhydrazine derivatives upon fine-tuning of the substrates and the reagent equivalency in a one-pot manner. The method was applied to the synthesis of active pharmaceutical ingredients of therapeutic drugs such as isocarboxazid.

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Can You Really Do Chemisty Experiments About 4-Amino-1-methylpiperidine

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Aminohaloborane in Organic Synthesis. IX. Exclusive ortho Acylation Reaction of N-Monoaminoalkylanilines

The exclusive ortho acylation reaction of aniline derivatives using boron trichloride made possible the one-step synthesis of 2-acyl-N-monoaminoalkylanilines (1) and the corresponding imines (2) from N-monoaminoalkylanilines, even in the case of compounds with a bulky substituent at the nitrogen atom.Conventional methods only give 1 via elaborate procedures.Keywords: regioselective reaction; 2-acylaniline derivative; 2-acylaniline-imine derivative; boron trichloride

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Brief introduction of 934536-10-4

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NEW PYRIDOPYRIMIDINES DERIVATIVES COMPOUNDS

The present invention describes new pyridopyrimidine derivatives compounds with structure represented by General Formula (I): or pharmaceutically acceptable salts thereof, or their mixtures (in any ratio), a pharmaceutical composition containing them, a method for using the new pyridopyrimidine derivatives compounds as inhibitor of the cyclic nucleotide synthesis or as inhibitor of the cAMP and cGMP synthesis, and their uses in the prophylactic and/or curative treatment of diarrhea, colitis and irritable bowel syndrome.

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Piperidine | C5H17669N – PubChem

 

Awesome and Easy Science Experiments about 6789-94-2

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SYNTHESIS OF PIPERIDINE DERIVATIVES AS POTENTIAL ANALGETIC AGENTS

Reaction of N-(1-(2-phenylethyl)-4-piperidinyl)propionanilide (I) with phosphorus pentasulfide gave the thioamide VI.Acylation of N-(1-(2-phenylethyl)-4-piperidinyl)aniline with 2-(methoxy)acetic and 2-(methylthio)acetic anhydrides afforded the amides II and III.Treatment of 4-anilino-1-benzylpiperidine-4-methanol with thionyl chloride gave the spirocyclic sulfurous acid ester amide XIV.Reduction of the hydrochloride of ethyl 3-(1-ethoxycarbonyl-4-phenylimino-3-piperidinyl)propionate (XXII) with sodium cyanoborohydride gave the perhydro-1,6-naphthyridine derivative XIX, a model compound in the synthesis of the cyclic analogue of fentanyl (I).Ethyl 4-anilino-1-(2-phenylethyl)-1,2,3,6-tetrahydropyridine-3-carboxylate (XXIX) hydrochloride, obtained by reaction of ethyl 4-oxo-1-(2-phenylethyl)piperidine-3-carboxylate hydrochloride with aniline, was reduced with lithium aluminium hydride to 4-anilino-1-(2-phenylethyl)piperidine-3-methanol (XXXI). 1-Methyl- and 1-benzyl-4-piperidone were reacted with 4-cyclopropylphenylmagnesium bromide and the tertiary alcohols XXXVII and XXXVIII obtained were acylated with propionyl chloride to give the esters XXXIX and XL.The piperidine derivatives XLI, XLVI and XLVIII were prepared as potential neurotropic agents.Alkylation of 8-hydroxy-6,11-dimethyl-1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocine (XLIX) with 2-(2-chloroethyl)-1,3-dioxane and -1,3-dioxolane resulted in the 6,7-benzomorphan derivatives L and LI.Out of the compounds prepared, only the closest fentanyl analogues II, III, and VI showed very strong analgetic activity.

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A new application about 77542-18-8

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MUSCARINIC RECEPTOR AGONISTS THAT ARE EFFECTIVE IN THE TREATMENT OF PAIN, ALZHEIMER’S DISEASE AND SCHIZOPHRENIA

Compounds of Formula IA, or pharmaceutically acceptable salts thereof: IA wherein G1, G2, G3, G4, R1, R2, X, Y, Z and n are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.

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Extended knowledge of 203661-69-2

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CYCLIC COMPOUNDS AS IMMUNOMODULATING AGENTS

The present disclosure describes novel IDO inhibitors and methods for preparing them. The pharmaceutical compositions comprising such IDO inhibitors and methods of using them for treating cancer, infectious diseases, and other disorders are also described

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The Absolute Best Science Experiment for 2-(4,4-Difluoropiperidin-1-yl)ethanamine

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Application of 605659-03-8, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.605659-03-8, Name is 2-(4,4-Difluoropiperidin-1-yl)ethanamine, molecular formula is C7H14F2N2. In a article£¬once mentioned of 605659-03-8

FUSED HETEROCYCLYC INHIBITOR COMPOUNDS

The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) and/or Cyclin-dependent kinase (CDK) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound

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Robust and Scalable Approach to 1,3-Disubstituted Pyridylcyclobutanes

An approach to all isomeric 3-pyridylcyclobutane-derived building blocks, i.e. ketones, alcohols and amines, is described. Synthesis of the title compounds relied on the five-step reaction sequence including alkylation of isomeric pyridyl acetonitriles with 1,3-dibromo-2,2-dimethoxypropane. Hydrolysis, decarboxylation and removal of the ketal moiety led to the key 3-pyridylcyclobutanones (obtained on up to 120 g scale in a single run), which were transformed into the corresponding alcohols and amines with high diastereoselectivity. The title cyclobutanone derivatives were used to synthesize three isomeric nicotine analogues, as well as for parallel synthesis of a small lead-like compound library via reductive amination.

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Final Thoughts on Chemistry for (S)-tert-Butyl (piperidin-2-ylmethyl)carbamate

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Synthetic Route of 139004-93-6, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.139004-93-6, Name is (S)-tert-Butyl (piperidin-2-ylmethyl)carbamate, molecular formula is C11H22N2O2. In a Article£¬once mentioned of 139004-93-6

Triazolinone Biphenylsulfonamide Derivatives as Orally Active Angiotensin II Antagonists with Potent AT1 Receptor Affinity and Enhanced AT2 Affinity

Several series of 2,4-dihydro-2,4,5-trisubstituted-3H-1,2,4-triazol-3-ones with acidic sulfonamide replacements of tetrazole at the 2′-position of the biphenyl-4-ylmethyl side chain at N4 were prepared and tested as angiotensin II (AII) antagonists.Preferred substituents on the triazolinone ring were n-butyl at C5 and 2-(trifluoromethyl)phenyl at N2.Subnanomolar IC50 values at the AT1 receptor subtype were observed for a variety of acylsulfonamides, including aroyl, heteroaroyl, and cycloalkylcarbonyl derivatives.Certain other acidic sulfonamides, such as sulfonylcarbamates and disulfimides also displayed high affinity for the AT1 receptor.In addition, AT2 binding for some of these compounds was increased by as much as 1000-fold over the corresponding tetrazole (e.g., AT2 IC50 17 nM for the tert-butyl sulfonylcarbamate 92).When evaluated for inhibition of the AII pressor response, the benchmark benzoylsulfonamide 9 (L-159,913) was efficacious in several species and was superior to losartan (1a) in conscious rhesus monkeys.Several subsequent analogues, including the 2-chlorobenzoyl (18), (3-chlorothiophene-2-yl)carbonyl (51), ((S)-2,2-dimethylcyclopropyl)carbonyl (80), and tert-butoxycarbonyl (92) derivatives, were highly effective in rats, surpassing 9 and losartan in duration of action and/or potency.Compound 18 (L-162,223) displayed very prolonged AII antagonism in the rat model (>24 h at 1 mg/kg iv).At 1 mg/kg po in rats, 18 and 92 (L-162,234) produced 85-87percent peak inhibition of the AII pressor response with duration exceeding 6 h.The identification of triazolinone-based sulfonamide derivatives combining high AT1 affinity, considerably enhanced AT2 potency, and favorable in vivo properties provides insights relevant to the design of dual AT1/AT2 receptor antagonists.

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Piperidine | C5H16767N – PubChem