32989-56-3

Upstream product

• 89-59-8 4-chloro-2-nitrotoluene 
• 4637-24-5 N,N-dimethyl-formamide dimethyl acetal 
• 5815-08-7 tert-Butoxybis(dimethylamino)methane 

Downstream Products

• 5551-11-1 4-Chloro-2-nitrobenzaldehyde 
• 81321-71-3 3-Bromomethyl-4-(2,4-dichloro-phenyl)-1-(4-fluoro-phenyl)-1H-pyrazole 
• 81321-62-2 [4-(2,4-Dichloro-phenyl)-1-(4-fluoro-phenyl)-1H-pyrazol-3-yl]-methanol 
• 81321-79-1 [4-(2,4-Dichloro-phenyl)-1-(4-fluoro-phenyl)-1H-pyrazol-3-yl]-acetonitrile 
• 77443-11-9 [4-(2,4-Dichloro-phenyl)-1-(4-fluoro-phenyl)-1H-pyrazol-3-yl]-acetic acid 
• 81321-54-2 4-(2-Amino-4-chlorphenyl)-1-(4-fluorphenyl)-pyrazol-3-carbonsaeure-ethylester 
• 81321-50-8 4-(2,4-Dichlorphenyl)-1-(4-fluorphenyl)-pyrazol-3-carbonsaeure-ethylester 
• 81321-53-1 4-(4-Chlor-2-nitrophenyl)-1-(4-fluorphenyl)-pyrazol-3-carbonsaeure-ethylester 
• 1269632-26-9 methyl (2E)-3-[2-(4'-chloro-2'-nitrostyryl)-1-(phenylsulfonyl)indol-3-yl]but-2-enoate 
• 69111-49-5 2-nitro-4-chlorophenylacetaldehyde 
• 223787-61-9 N-{2-[2-(2-bromo-4-chloro-phenyl)-ethyl]-5-chloro-phenyl}-formamide 
• 223787-55-1 2-[2-(2-bromo-4-chloro-phenyl)-ethyl]-5-chloro-phenylamine 
• 223787-50-6 C₁₄H₈BrCl₂NO₂ 
• 78347-96-3 diethyl <(2-bromo-4-chlorophenyl)methyl>phosphonate 

Relevant academic research and scientific papers

CuH-Catalyzed Enantioselective Alkylation of Indole Derivatives with Ligand-Controlled Regiodivergence

Enantioenriched molecules bearing indole-substituted stereocenters form a class of privileged compounds in biological, medicinal, and organic chemistry. Thus, the development of methods for asymmetric indole alkylation is highly valuable in organic synthesis. Traditionally, achieving N-selectivity in indole alkylation reactions is a significant challenge, since there is an intrinsic preference for alkylation at C3, the most nucleophilic position. Furthermore, selective and predictable access to either N- or C3-alkylated chiral indoles using catalyst control has been a long-standing goal in indole functionalization. Herein, we report a ligand-controlled regiodivergent synthesis of N- and C3-alkylated chiral indoles that relies on a polarity reversal strategy. In contrast to conventional alkylation reactions in which indoles are employed as nucleophiles, this transformation employs electrophilic indole derivatives, N-(benzoyloxy)indoles, as coupling partners. N- or C3-alkylated indoles are prepared with high levels of regio- and enantioselectivity using a copper hydride catalyst. The regioselectivity is governed by the use of either DTBM-SEGPHOS or Ph-BPE as the supporting ligand. Density functional theory (DFT) calculations are conducted to elucidate the origin of the ligand-controlled regiodivergence.

A depression drug impurity of preparing method (by machine translation)

The invention relates to a depression drug impurity of preparing method, it comprises the following steps: (a) the high sodium iodate, water and mixed DMF; (b) is poured into ice water, adjusting pH with alkali and layered extraction, purification to obtain compound 4; in the 120 - 150 °C reaction after column chromatography separation to obtain compound 5; (c) the compound 3 and said compound 5 by adding ethylene glycol dimethyl ether, in the ice water bath under the conditions of the adding sodium hydride to, heating up to 40 - 60 °C reaction 20 - 40 minutes, further heating up to reflux; (d) the compound 6 with the [...] catalyst, morpholine, methanol and ethanol are mixed, the reaction is carried out in a hydrogen atmosphere, filtered [...] filtrate to obtain compound 7; (e) the compound 7 with formic acid, a sodium mixed, heated to 100 - 120 °C refluxing reaction; (g) the compound 10 in toluene soluble, in an inert gas atmosphere by adding sodium hydride, temperature reaction. This can obtain the high purity of the depression drug impurity isomer, for impurity accurate control. (by machine translation)

Preparation method of impurity isomer key intermediate of anti-depressive drug

The invention relates to a preparation method of an impurity isomer key intermediate of an anti-depressive drug. The preparation method comprises the following steps: (a) mixing sodium periodate, water and DMF (Dimethylformamide); (b) pouring in ice water, adjusting pH with an alkaline solution, extracting by layers, purifying to obtain a compound 4, and performing column chromatography isolationafter reacting at 120 to 150 DEG C to obtain a compound 5; (c) adding the compound 3 and the compound 5 into 1,2-dimethoxyethane, adding sodium hydride under the condition of ice water bath, heating to 40 to 60 DEG C for reacting for 20 to 40 minutes, and heating and refluxing; (d) mixing the compound 6 with a rhodium carbon catalyst, morpholine, methanol and ethanol, reacting under a hydrogen atmosphere, and performing suction filtration and spin drying on filtrate to obtain a compound 7; (e) mixing the compound 7 with formic acid and sodium formate, and heating to 100 to 120 DEG C for refluxreaction; (f) adding anhydrous K2CO3,Cu powder and CuBr, performing reaction under the protection of insert gas at the temperature of 150 to 180 DEG C to obtain a compound 9; cooling to 30 to 60 DEGC, adding NaOH solution to perform reaction, filtering, and purfying to obtain a compound 10.. By adopting the preparation method, a high-purity impurity isomer of the anti-depressive drug can be obtained for accurate control of impurities.

Preparation method of chloronitrophenyl intermediate serving as impurity isomer of medicine for treating depression

The invention relates to a preparation method of a chloronitrophenyl intermediate serving as an impurity isomer of medicine for treating depression. The method includes the following steps that a, sodium periodate, water and DMF are mixed, then a DMF solution of a compound 2 is added for a reaction, and after the reaction, a filtrate is taken and purified to obtain a compound 3; b, 2-bromo-4-chlorotoluene, N-bromosuccinimide, dibenzoyl peroxide and carbon tetrachloride are mixed, stirred, heated to 80-100 DEG C for a reaction and then poured into ice water, the pH is adjusted with lye, and layered extraction and purification are conducted to obtain a compound 4; c, the compound 3 and a compound 5 are added into glycol dimethyl ether, sodium hydride is added under the condition of an ice water bath, the temperature is raised to 40-60 DEG C for a reaction for 20-40 minutes, then the temperature is raised for reflux, after the reaction is completed, water and ethyl acetate are added in avolume ratio of 1:1, and solid is precipitated, subjected to suction filtration and dried to obtain a compound 6. In this way, the nitrophenyl intermediate with high purity can be obtained to be usedfor subsequent preparation of the high-purity and high-yield impurity isomer of medicine for treating depression.

ALPHA 7 NICOTINIC ACETYLCHOLINE ALLOSTERIC MODULATORS, THEIR DERIVATIVES AND USES THEREOF

The present application is related to compounds represented by Formula I, which are novel positive allosteric modulators of al nAChRs. The application also discloses the treatment of disorders that are responsive to enhancement of acetylcholine action on al nAChRs in a mammal by administering an effective amount of a compound of Formula I.

Synthetic studies on indolocarbazoles: Total synthesis of staurosporine aglycon

A synthesis of staurosporine aglycon and its analogs was achieved in a 28-36% overall yield starting from 2-methylindole. The prominent key steps for the synthesis of the indolocarbazole alkaloids involved electrocyclization and nitrene insertion reactions.

Facile, environmentally friendly synthesis of benzaldehyde and phenylacetaldehyde analogs from readily available toluene derivatives

A facile environmentally friendly synthesis of bezaldehyde and phenylacetaldehyde analogs from readily available toluene derivatives is described. Oxidation of the styrylamines by H2O2 H2O2 affords benzaldehydes in moderate yields, while the hydrolysis of styrylamines afforded phenylacetaldehyde analogs in good yields. Copyright

Convenient modification of the Leimgruber-Batcho indole synthesis: Reduction of 2-nitro-p-pyrrolidinostyrenes by the FeCl3-activated carbon-N2H4H2O system

A new catalytic system containing ferric chloride, activated carbon, and hydrazine has been proposed for the reductive cyclization of β-dialkylamino-2-nitrostyrenes to give the corresponding indoles (Leimgruber-Batcho synthesis). Various substituted indoles may be obtained in high yield under these conditions.

HETEROCYCLIC INHIBITORS OF HISTAMINE RECEPTORS FOR THE TREATMENT OF DISEASE

The present invention relates to compounds and methods which may be useful as inhibitors of H1R and/or H4R for the treatment or prevention of inflammatory, autoimmune, allergic, and ocular diseases.

HETEROCYCLIC INHIBITORS OF HISTAMINE RECEPTORS FOR THE TREATMENT OF DISEASE

The present invention relates to compounds and methods which may be useful as inhibitors of H1R and/or H4R for the treatment or prevention of inflammatory, autoimmune, allergic, and ocular diseases.