cas 149947-15-9, 2-BROMO-3-FLUOROBENZALDEHYDE

Articles about 149947-15-9Total 13 be found

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Enantioselective Total Synthesis of Beraprost Using Organocatalyst
A convergent and enantioselective total synthesis of the most active isomer of beraprost was achieved in 17 pots. A unique tricyclic core in beraprost was synthesized efficiently by utilizing the asymmetric organocatalyst-mediated formal [3 + 2] cycloaddi
Umemiya, Shigenobu,Sakamoto, Daisuke,Kawauchi, Genki,Hayashi, Yujiro
p. 1112 - 1115
(2017)
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Method for rapidly synthesizing 3-bromo-2-fluorobenzaldehyde based on continuous flow reaction technology
The invention discloses a method for rapidly synthesizing 3-bromine-2-fluorobenzaldehyde based on a continuous flow reaction technology. The method comprises a lithium-hydrogen exchange reaction and a nucleophilic hydroformylation reaction, wherein the lithium-hydrogen exchange reaction comprises the following steps: pumping an o-fluorobromobenzene solution and an organic lithium reagent solution into a lithium-hydrogen exchange continuous reactor according to a certain equivalent proportion; reacting for a certain time at a certain temperature, and carrying out lithium-hydrogen exchange to generate a 3-bromo-2-fluorophenyl lithium intermediate; and the nucleophilic hydroformylation reaction comprises the steps: introducing the active intermediate obtained in the lithium-hydrogen exchange reaction into a hydroformylation continuous reactor, pumping N, N-dimethylformamide in a certain equivalent proportion into the hydroformylation continuous reactor, and reacting at a certain temperature for a certain time to generate a 3-bromo-2-fluorobenzaldehyde product. By applying the continuous flow reaction technology, the traditional kettle type reaction is improved into a continuous process, the amplification effect problem of the traditional kettle type reaction is solved, the danger level of the dangerous reaction of the metal-containing reagent is reduced, the reaction can obtain higher product purity under the controllable continuous condition, and the production efficiency is improved.
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Paragraph 0008; 0019-0022

(2021/08/19)

THIAZOLOPYRIMIDINONES AS MODULATORS OF NMDA RECEPTOR ACTIVITY
The present invention relates to certain thiazolopyrimidinone compounds for use in modulating NMDA receptor activity, pharmaceutical compositions comprising such compounds and methods of treating neurological and psychiatric conditions.
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Paragraph 0379

(2015/04/28)

N-(piperidin-4-yl)benzo[b]thiophenecarboxamide derivatives, preparation method therof, and pharmaceutical composition for use in preventing or treating Urotensin-Ⅱ receptor activity related diseases containing the same as an active ingredient
The present invention relates to N-(piperidin-4-yl)benzo[b]thiophenecarboxamide derivatives, a manufacturing method thereof, and a pharmaceutical composition for preventing or treating urotensin-II receptor activity-related diseases comprising the same as an active ingredient. The N-(piperidin-4-yl)benzo[b]thiophenecarboxamide derivatives can be usefully used for preventing or treating urotensin-II receptor activity-related diseases such as congestive heart failure, ischemic heart, myocardial infarction, cardiomegaly, fibrosis cordis, coronary artery disease, arteriosclerosis, hypertension, asthma, renal failure, diabetes, vasculitis, neurodegenerative disease, stroke, pain, depressive disorder, psychosis, cancer, etc., by acting as an antagonist with respect to a urotensin-II receptor.COPYRIGHT KIPO 2016
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Paragraph 0181; 0182; 0183; 0184

(2016/10/10)

SULPHONYLAMINOPYRROLIDINONE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION
The invention relates to new sulphonylaminopyrrolidinone compounds having antithrombotic activity which, in particular, inhibit blood clotting factor IXa and/ or factor Xa, to processes for their preparation and to use thereof as drugs.
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Page/Page column 42; 43

(2013/07/05)

Compounds and Methods for Inhibiting the Interaction of BCL Proteins with Binding Partners
The invention relates to isoxazolidine containing compounds that bind to bcl proteins and inhibit Bcl function. The compounds may be used for treating and modulating disorders associated with hyperproliferation, such as cancer.
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Page/Page column 120

(2008/12/05)

Polyfluorinated fused aromatics and their use in liquid-crystal mixtures
A compound of the formula (I) is described where: R1 is a) H b) a straight-chain or branched alkyl radical having from 1 to 16 carbon atoms or a straight-chain or branched alkenyl radical having from 2 to 16 carbon atoms, in which b1) one or more nonadjacent and nonterminal CH2 groups may be replaced by —O—, —C(═O)O—, —O—C(═O)—, —O—C(═O)—O—, —C(═O)— or —Si(CH3)2— and/or b2) one CH2 group may be replaced by —C≡C—, cyclopropane-1,2-diyl, cyclobutane-1,3-diyl, cyclohexane-1,4-diyl or phenylene-1,4-diyl and/or b3) one or more hydrogen atoms may be replaced by F and/or Cl c) -M1-A1-R5 R2 has the same possible definitions as specified for R1, with the exception of H, but independently of the definition of R1 and R5 R5 has the same possible definitions as specified for R1, with the exception of -M1-A1-R5, but independently of the definition of R1 and R3 M1 is —CO—O—, —O—CO—, —CH2—O—, —O—CH2—, —CF2—O—, —O—CF2—, —CH═CH—, —CF═CF—, —C≡C—, —CH2—CH2—CO—O—, —O—CO—CH2—CH2—, —CH2—CH2—, —CF2—CF2—, —(CH2)4—, —OC(═O)CF═CF— or a single bond A1 is 1,4-phenylene in which one or two hydrogen atoms may be replaced by F, Cl, CN and/or OCF3 or three hydrogen atoms may be replaced by fluorine, 1,4-cyclohexylene in which one or two hydrogen atoms may be replaced by CH3 and/or F, 1-cyclohexene-1,4-diyl in which one hydrogen atom may be replaced by CH3 or F, pyrimidine-2,5-diyl, pyridine-2,5-diyl in which one hydrogen atom may be replaced by F, or 1,3-dioxane-2,5-diyl p, q, rare each independently 0 or 1, i.e. at the value zero, —H is present at the appropriate position instead of —F, with the proviso that: at least one of p, q, r is 1.
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(2008/06/13)

POLYFLUORINATED CONDENSED AROMATIC COMPOUND AND USE THEREOF IN LIQUID CRYSTAL MIXTURE
PROBLEM TO BE SOLVED: To provide a polyfluorinated condensed aromatic compound and a liquid crystal mixture. SOLUTION: The liquid crystal mixture contains a compound of formula (I) [wherein, for example, R1 is H, propyl or butyloxy; R2 is propyl; p and q are each 1; and r is 0 or 1].
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Page/Page column 17

(2010/02/15)

Cyclocarbamate derivatives as progesterone receptor modulators
This invention provides compounds of Formula (I): wherein R1 and R2 may be single substituents or fused to form spirocyclic or hetero-spirocyclic rings; R3 is H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituted C1 to C6 alkenyl, alkynyl, or substituted alkynyl, CORC; RC is H, C1 to C3 alkyl, substituted C1 to C3 alkyl, aryl, substituted aryl, C1 to C3 alkoxy, substituted C1 to C3 alkoxy, C1 to C3 aminoalkyl, or substituted C1 to C3 aminoalkyl; R4 is H, halogen, CN, NO2, C1 to C6 alkyl, substituted C1 to C6 alkyl, alkynyl, or substituted alkynyl, C1 to C6 alkoxy, substituted C1 to C6 alkoxy, amino, C1 to C6 aminoalkyl, or substituted C1 to C6 aminoalkyl; and R5 is selected from a trisubstituted benzene ring of a five or six membered ring with 1, 2, or 3 heteroatoms from the group including O, S, SO, SO2 or NR6 and containing one or two independent substituents from the group including H, halogen, CN, NO2, amino, and C1 to C3 alky, C1 to C3 alkoxy, C1 to C3 aminoalkyl, CORF, or NRGCORF; or pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and methods using the compounds as antagonists of the progesterone receptor.
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(2008/06/13)

Indoline derivatives
This invention relates to substituted indoline derivative compounds which are antagonists of the progesterone receptor, their preparation and pharmaceutical utility, particularly including contraception and treatment of benign or malignant neoplastic diseases, having the general structure: wherein R1and R2may be single substituents or fused to form spirocyclic rings.
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(2008/06/13)

Combination regimens using progesterone receptor modulators
This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds which are antagonists of the progesterone receptor having the general structure: wherein R1and R2may be single substituents or fused to form spirocyclic or hetero-spirocyclic rings; R3is H, OH, NH2, C1to C6alkyl, substituted C1to C6allyl C3to C6alkenyl, substituted C1to C6alkenyl, alkynyl, or substituted alknyl, CORC; RCis H, C1to C3alkyl, substituted C1to C3alkyl, aryl, substituted aryl, C1to C3alkoxy, substituted C1to C3alkoxy, C1to C3aminoalkyl, or substituted C1to C3aminoalkyl; R4is H, halogen, CN, NO2, C1to C6alkyl, substituted C1to C6alkyl alkynyl, or substituted alkynyl, C1to C6alkoxy, substituted C1to C6alkoxy, amino, C1to C6aminoalkyl, or substituted C1to C6aminoalkyl; and R5is selected from a trisubstituted benzene ring of a five or six membered ring with 1, 2, or 3 heteroatoms from the group including O, S, SO, SO2or NR6and containing one or two independent substituents from the group including H, halogen, CN, NO2, amino, and C1to C3alkyl, C1to C3alkoxy, C1to C3aminoalkyl, CORF, or NRGCORF; or pharmaceutically acceptable salt thereof. These methods of treatment may be used for contraception or for the treatment and/or prevention of secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis; polycystic ovary syndrome, carcinomas and adenocarcinomas of the endometrium, ovary, breast, colon, prostate, or inmization of side effects or cyclic menstrual bleeding. Additional uses of the invention include stimulation of food intake.
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(2008/06/13)

CYCLIC REGIMENS UTILIZING INDOLINE DERIVATIVES
This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds which are antagonists of the progesterone receptor having the general structure: wherein R 1 and R 2 may be single substituents or fused to form spirocyclic rings, in combination with progestins, estrogens, or both. These methods of treatment may be used for contraception or for the treatment and/or prevention of secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis; polycystic ovary syndrome, carcinomas and adenocarcinomas of the endometrium, ovary, breast, colon, prostate, or minimization of side effects or cyclic menstrual bleeding. Additional uses of the invention include stimulation of food intake.
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(2008/06/13)

3,4-dihydro-4-oxo-3-(2-propenyl)-1-phthalazineacetic acids and derivatives, their preparations and medicines containing them
Novel 3,4-dihydro-4-oxo-3(prop-2-enyl)-1-phtalazineacetic acids and derivatives of formula (I) STR1 in which R1 R2 and R3 are the same or different and stand for H, a halogen or a linear or branched aliphatic, saturated or unsaturated radical, substituted or not by at least one halogen or R4 residue such as defined below, except when R4 is H; R4 and R5 are the same or different and stand for H, a linear or branched aliphatic radical, saturated or unsaturated, an aryl or heteroaryl radical, said radicals being substituted or not by at least one grouping such as fluorine, chlorine, bromine, methyl or trifluoromethyl, where R4 and R5 do not simultaneously denote H; R6 stands for hydroxy or alkoxy radical; R7 stands for H, a halogen, a linear or branched aliphatic saturated or unsaturated radical, an alkoxy radical, said radicals being substituted or not by analiphatic or halogenated radical, a nitro group, a substituted or unsubstituted amino group, S(O)n R8 or a cyano group; n is equal to 0,1 or 2; R8 is an aliphatic, linear or branched radical, an aryl or heteroaryl radical, an amino radical, said radicals being substituted or not by an aliphatic or halogenated radical. This invention also relates to the optional tautomeric forms of said acids and their pharmaceutically acceptable base addition salts. Also described is a process for preparing said compounds and the drugs containing same.
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(2008/06/13)