Category: 81616-80-0

On March 10, 1994, Achard, D.; Truchon, A.; Peyronel, J. F. published an article.Computed Properties of 81616-80-0 The title of the article was Perhydrothiopyranopyrroles derivatives: a novel series of potent and selective nonpeptide NK1 antagonists. And the article contained the following:

The synthesis of RP 73467 (I), a representative of 4,4-di-Ph perhydrothiopyrano[2,3-c]-pyrrole-1-oxides, a new series of potent and selective nonpeptide NK1 Substance P antagonists, is described. The experimental process involved the reaction of (S)-2-(2-Methoxyphenyl)propanoic acid(cas: 81616-80-0).Computed Properties of 81616-80-0

The Article related to perhydrothiopyranopyrrole derivative nk1 receptor antagonist preparation, Pharmacology: Structure-Activity and other aspects.Computed Properties of 81616-80-0

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On July 22, 1994, Garret, Claude; Montier, Francois published a patent.HPLC of Formula: 81616-80-0 The title of the patent was Pharmaceutical compositions containing synergistic Nk1 and NK2 receptor antagonists. And the patent contained the following:

Pharmaceutical compositions containing synergistic Nk1 and NK2 receptor antagonists are used for the treatment of diseases caused by substance P and/or neurokinine A. I.v. injection of [imino-1-(methoxy-2-phenyl)-2-ethyl]-2-diphenyl-7,7-perhydroisoindolone-4-(3aR,7aR) (preparation given) and N-methyl[(phenyl-4-acetamido-4-piperidinyl)-4-(dichloro-3,4-phenyl)-2-butyl]benzamide (I) at 0.5mg/kg did not inhibit the capsaicin-induced bladder contractions in rats, while the combination of both decreased the contractions by 74%. A tablet contained [diphenyl-7,7-(methoxy-2-phenyl)-2-propionyl-(S)]-2-perhydroisoindolol-4-(3aS,4S, 7aS) 12.5, I 12.5, starch 83, silica 30, and Mg stearate 3 mg. The experimental process involved the reaction of (S)-2-(2-Methoxyphenyl)propanoic acid(cas: 81616-80-0).HPLC of Formula: 81616-80-0

The Article related to pharmaceutical synergism nk1 nk2 receptor antagonist, tablet synergism nk1 nk2 receptor antagonist, Pharmaceuticals: Formulation and Compounding and other aspects.HPLC of Formula: 81616-80-0

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On July 2, 1982, Brown, John M.; Parker, David published an article.Synthetic Route of 81616-80-0 The title of the article was Mechanism of asymmetric hydrogenation. Rhodium complexes formed by unsaturated carboxylic acids, carboxylates, and carboxamides. And the article contained the following:

��Unsaturated acids displace solvent from (R,R)-I (L = MeOH) cation, forming chelate complexes in which olefin and carboxylate are bound to the metal. The strength of complexation is enhanced in basic media and propenoic or 2-methylpropenoic acid form a different type of species with 2:1 stoichiometry in the absence of base. ��And ��unsaturated amides likewise form complexes in which olefin and carboxamide O are bound to Rh. The ratio of diastereomers observed by 31P NMR does not correlate with optical yields in hydrogenation of these precursors. In related experiments with (R,R)-[1,2-bis(o-anisylphenylphosphino)ethane]bis(methanol)rhodium cation, 2-methylenesuccinic acid and its Me esters gave a variety of complexes, including tridentate species where both carboxyl groups and olefin were concomitantly bound. The experimental process involved the reaction of (S)-2-(2-Methoxyphenyl)propanoic acid(cas: 81616-80-0).Synthetic Route of 81616-80-0

The Article related to asym hydrogenation rhodium complex, rhodium carboxylate carboxamide complex, olefin rhodium complex, Organometallic and Organometalloidal Compounds: Group Viii – Co, Ni, Ru, Rh, Pd, Os, Ir, Pt and other aspects.Synthetic Route of 81616-80-0

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On November 25, 1996, Mutti, Stephane; Daubie, Christophe; Malpart, Joel; Radisson, Xavier published an article.Related Products of 81616-80-0 The title of the article was Practical enantiospecific synthesis of RPR 111905, a novel non-peptide substance P antagonist. And the article contained the following:

The synthesis of enantiomerically pure RPR 111905 (I) was achieved in twelve steps with an overall yield of 6.9%. The synthetic strategy was based on a Diels-Alder reaction to generate the bicyclic framework and the asymmetry was introduced by resolution The experimental process involved the reaction of (S)-2-(2-Methoxyphenyl)propanoic acid(cas: 81616-80-0).Related Products of 81616-80-0

The Article related to rpr 111905 enantiospecific preparation, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Related Products of 81616-80-0

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On April 13, 1995, Garret, Claude; Louvel, Erik published a patent.Recommanded Product: (S)-2-(2-Methoxyphenyl)propanoic acid The title of the patent was Preparation of perhydroisoindole antiemetics. And the patent contained the following:

The title compounds [I; R = (un)substituted Ph; R1 = (un)substituted Ph, cyclohexadienyl, naphthyl, indenyl, (un)substituted heterocyclyl; R2 = H, halogen, OH, alkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkyloxy, alkylthio, acyloxy, CO2H, (un)substituted alkyloxycarbonyl, benzyloxycarbonyl, NH2, acylamino; R3 = (un)substituted Ph; R4 = OH or F if R5 = H; etc.] [e.g., (3aS,4S,7aS)-7,7-diphenyl-4-(2-methoxyphenyl)-2-tert-butoxycarbonyl-4-perhydroisoindolol], useful as antiemetics, are prepared and I-containing formulations presented. The experimental process involved the reaction of (S)-2-(2-Methoxyphenyl)propanoic acid(cas: 81616-80-0).Recommanded Product: (S)-2-(2-Methoxyphenyl)propanoic acid

The Article related to perhydroisoindole preparation antiemetic, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Recommanded Product: (S)-2-(2-Methoxyphenyl)propanoic acid

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Ether – Wikipedia,
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On November 19, 1992, Achard, Daniel; Grisoni, Serge; Hanessian, Stephen; Moutonnier, Claude; Peyronel, Jean Francois; Tabart, Michel; Truchon, Alain published a patent.Electric Literature of 81616-80-0 The title of the patent was Preparation of N-acyltetrahydroisoindoles as drugs. And the patent contained the following:

Title compounds [I; R1 = H; R1R1 = bond; R2 = Ph, halophenyl, tolyl; R3 = halo, OH; R4 = H, halo; R5 = C(:X)CHRR’; R = Ph, alkyl, alkoxy, heterocyclyl, etc.; R’ = H, halo, OH, alkyl, etc.; X = O, NH] were prepared as substance P antagonists (no data). Thus, 4,4-diphenyl-2-cyclohexenone was cyclocondensed with PhCH2N(CH2OBu)CH2SiMe3 and the product converted in 7 steps to fluorotetrahydroisoindole (R,R,R)-II (III; R5 = H) which was N-acylated by 2-[Me2N(CH2)3O]C6H4CH2CO2H (preparation given) to give III.HCl [R5 = COCH2C6H4[O(CH2)3NMe2]-2]. The experimental process involved the reaction of (S)-2-(2-Methoxyphenyl)propanoic acid(cas: 81616-80-0).Electric Literature of 81616-80-0

The Article related to isoindole acyltetrahydro substance p antagonist, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Electric Literature of 81616-80-0

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On June 5, 1991, Dubroeucq, Marie Christine; Moutonnier, Claude; Peyronel, Jean Francois; Tabart, Michel; Truchon, Alain published a patent.Category: ethers-buliding-blocks The title of the patent was Isoindolone derivatives, useful as intermediates for substance P antagonists, and their preparation. And the patent contained the following:

Title compounds I [both R = H; or RR = bond; R1 = H, easily removed radical; R2 = (identically) Ph substituted optionally by halo or Me in ortho or meta position] (II), especially the (3aRS,7aRS)- and (3aR,7aR)-isomers, are prepared as intermediates for I [R1 = C(X)CHR3R4; X = O, S, NR5; R3 = (substituted) Ph, cyclohexadienyl, naphthyl, heterocyclyl; R4 = H, halo, OH, alkyl, aminoalyl, alkoxy, CO2H, amino, etc.; R5 = H, (substituted) alkyl, dialkylamino] (III), which are antagonists of substance P (no data) were prepared Cyclocondensation of 4,4-diphenyl-2-cyclohexen-1-one with PhCH2N(CH2OBu)CH2SiMe3 in CH2Cl2 in the presence of CF3CO2H gave (3aRS,7aRS)-I (R = H, R1 = CH2Ph, R2 = Ph); this was debenzylated by H over Pd/C in MeOH-HCl and the product (R2 = H) amidated by PhCH2CO2H using N,N’-carbonyldiimidazole and Et3N in CH2Cl2 to give (3aRS,7aRS)-I (R = H, R1 = COCH2Ph, R2 = Ph). Seventeen syntheses of II and 24 of III are described. The experimental process involved the reaction of (S)-2-(2-Methoxyphenyl)propanoic acid(cas: 81616-80-0).Category: ethers-buliding-blocks

The Article related to isoindolone intermediate substance p antagonist, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Category: ethers-buliding-blocks

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On March 10, 1994, Tabart, M.; Peyronel, J. F. published an article.Application of 81616-80-0 The title of the article was Synthesis of RPR 100893, prototype of a new series of potent and selective nonpeptide NK1 antagonists: the triarylperhydroisoindolols. And the article contained the following:

The synthesis of enantiomerically pure RPR 100893 [(3aS,4S,7aS)-I] was described. One step involved coupling of 2 chiral moieties by an acylation reaction. The experimental process involved the reaction of (S)-2-(2-Methoxyphenyl)propanoic acid(cas: 81616-80-0).Application of 81616-80-0

The Article related to rpr100893 enantiomer, isoindolol triarylperhydro, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Application of 81616-80-0

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On November 19, 1992, Achard, Daniel; Grisoni, Serge; Hanessian, Stephen; Moutonnier, Claude; Peyronel, Jean Francois; Tabart, Michel; Truchon, Alain published a patent.Quality Control of (S)-2-(2-Methoxyphenyl)propanoic acid The title of the patent was Perhydroisoindoles, their preparation and pharmaceutical compositions containing them as substance P antagonists. And the patent contained the following:

Perhydroisoindole derivatives I [R = H or form a bond; R5 = 2- or 3-halo- or Me-substituted Ph; Z = O, NH; R1 = (un)substituted Ph, cyclohexadienyl, naphthyl, heterocyclyl; R2 = H, halo, OH, alkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkoxy, alkylthio, acyloxy, carboxy, (un)substituted alkoxycarbonyl, benzyloxycarbonyl, amino, acylamino; R3 = halide, OH; R4 = H, or halo if R3 = halo] and their salts, prepared by reaction of R1CHR2CO2H or R1CHR2CR6:NH (R6 = C1-4 alkoxy, MeS, EtS, PhCH2S, alkoxycarbonylmethylthio) with the corresponding perhydroisoindoles, are claimed. The preparation of isomers of I, mixtures of isomers, and their salts are claimed. The compounds are particularly interesting as substance P antagonists; tests of 3 compounds, and 29 synthetic examples are described. The experimental process involved the reaction of (S)-2-(2-Methoxyphenyl)propanoic acid(cas: 81616-80-0).Quality Control of (S)-2-(2-Methoxyphenyl)propanoic acid

The Article related to perhydroisoindole preparation substance p antagonist, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Quality Control of (S)-2-(2-Methoxyphenyl)propanoic acid

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On October 13, 1994, Crespo, Andre; Fardin, Veronique; Guillaume, Jean-Marc; Malleron, Jean -Luc; Peyronel, Jean-Francois published a patent.Application of 81616-80-0 The title of the patent was Preparation of pharmaceutical perhydroisoindole derivatives as neurokinin A antagonists. And the patent contained the following:

Title compounds I (R = (substituted)Ph; R1 = (substituted)Ph, PhCh2O, (substituted)-C1-4 alkyl, (substituted)amino, (substituted)heterocyclyl, cyclohexadienyl, naphthyl, indenyl; R2 = H, halo, HO, alkyl, aminoalkyl, allylaminoalkyl, dialkylaminoalkyl, etc.; R3 = (substituted)Ph), are prepared (3AR,4R,5R,7aR)-7,7-diphenyl-4-(2-methoxyphenyl)perhydro-4,5-isoindolediol (preparation given) and 3-indolylacetic acid in CH2Cl2 were added to 1-benzotriazolylol hydrate, 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide and diisopropylethylamine to give (3aR,4R,5R,7aR)-I (R1 = 3-indolyl, R2 = H, R3 – 2-(MeO)C6H4) which at 10-1000 nM on human receptor NK2 showed IC50 of 215 nM. A formulation tablet comprising I is given. The experimental process involved the reaction of (S)-2-(2-Methoxyphenyl)propanoic acid(cas: 81616-80-0).Application of 81616-80-0

The Article related to arylperhydroisoindolediol preparation neurokinin antagonist, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Application of 81616-80-0

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Ether – Wikipedia,
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