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Related Products of 310466-38-7, 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.310466-38-7, Name is 4-Fluorobenzo[b]thiophene, molecular formula is C8H5FS. In a article£¬once mentioned of 310466-38-7

C17,20-lyase inhibitors I. Structure-based de novo design and SAR study of C17,20-lyase inhibitors.

Novel nonsteroidal C(17,20)-lyase inhibitors were synthesized using de novo design based on its substrate, 17 alpha-hydroxypregnenolone, and several compounds exhibited potent C(17,20)-lyase inhibition. However, in vivo activities were found to be short-lasting, and in order to improve the duration of action, a series of benzothiophene derivatives were evaluated. As a result, compounds 9h, (S)-9i, and 9k with nanomolar enzyme inhibition (IC(50)=4-9 nM) and 9e (IC(50)=27 nM) were identified to have powerful in vivo efficacy with extended duration of action. The key structural determinants for the in vivo efficacy were demonstrated to be the 5-fluoro group on the benzothiophene ring and the 4-imidazolyl moiety. Superimposition of 9k and 17 alpha-hydroxypregnenolone demonstrated their structural similarity and enabled rationalization of the pharmacological results. In addition, selected compounds were also identified to be potent inhibitors of human enzyme with IC(50) values of 20-30 nM.

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Benzothiophene – Wikipedia,
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Advances toward new antidepressants beyond SSRIs: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT1A receptor antagonism/SSRI activities. Part 2

Potent 5-HT1A/SSRIs at low nanomolar and subnanomolar concentrations were identified in a series of 1-(1H-indol-4-yloxy)-3-(4-benzo[b]thiophen-2-ylpiperidinyl)propan-2-ols. Incorporation of an alpha-Me group in the piperidine ring with its specific stereochemistry enhanced binding affinity at the 5-HT reuptake site and in vitro 5-HT1A antagonist functional activity.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 310466-38-7, and how the biochemistry of the body works.Electric Literature of 310466-38-7

Electric Literature of 310466-38-7, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.310466-38-7, Name is 4-Fluorobenzo[b]thiophene, molecular formula is C8H5FS. In a Patent£¬once mentioned of 310466-38-7

Dihydroimidazo[2,1-b]thiazole and dihydro-5h-thiazolo[3,2-A]pyrimidines as antidepressant agents

The present invention relates to certain novel substituted dihydroimidazo[2,1-b]thiazole and dihydro-5H-thiazolo[3,2-a]pyrimidine compounds of Formula (I) including pharmaceutically acceptable salts thereof in which have affinity for 5-HT1A receptors and which inhibits neuronal reuptake of 5-hydroxytryptamine and/or noradrenaline, to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, obesity, drug addiction, drug abuse, cognitive disorders, Alzheimer’s disease, obsessive-compulsive behaviour, panic attacks, social phobias, eating disorders such as bulimia, anorexia, snacking and binge eating, non-insulin dependent diabetes mellitus, hyperglycaemia, hyperlipidaemia, stress, as an aid to smoking cessation and in the treatment and/or prophylaxis of seizures, neurological disorders such as epilepsy and/or in which there is neurological damage such as stroke, brain trauma, cerebral ischaemia, head injuries and haemorrhage.

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Reference£º
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.310466-38-7, Name is 4-Fluorobenzo[b]thiophene, molecular formula is C8H5FS, 310466-38-7. In a Article, authors is Takeuchi, Kumiko£¬once mentioned of 310466-38-7

Advances toward new antidepressants beyond SSRIs: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT1A receptor antagonism/SSRI activities. Part 1

A series of 1-aryloxy-3-piperidinylpropan-2-ols possessing potent dual 5-HT1A receptor antagonism and serotonin reuptake inhibition was discovered. 1-(1H-Indol-4-yloxy)-3-(4-benzo[b]thiophen-2-ylpiperidinyl)propan-2-ols exhibited selective and high affinity at the 5-HT1A receptor and serotonin reuptake inhibition at nanomolar concentrations for dual activities.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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310466-38-7 4-Fluorobenzo[b]thiophene 19088017, abenzothiophene compound, is more and more widely used in various fields.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.310466-38-7,4-Fluorobenzo[b]thiophene,as a common compound, the synthetic route is as follows.

Example 5 4-Fluorobenzo[b]thiophene was prepared starting from methyl thioglycolate and 2,6-difluorobenzaldehyde and then following a similar procedure to that given for 4-bromobenzo[b]thiophene in Example 9. A solution of bromine (9.2 ml) in dichloromethane (200 ml) was added dropwise under nitrogen at -5 C. over 30 minutes to a stirred mixture of 4-fluorobenzo[b]thiophene (24.7 g), sodium acetate (20 g) and dichloromethane (200 ml). The mixture was stirred at ambient temperature for 24 hours, then it was filtered and the solvent was removed in vacuo. The residue was dissolved in dichloromethane (50 ml), water (200 ml) and zinc dust (34.3 g) were added, then the mixture was stirred and heated under reflux for 10 hours, cooled to ambient temperature and filtered through Celite. The Celite was washed with ethyl acetate (200 ml) then the combined organic solutions were washed with saturated aqueous sodium chloride solution (100 ml), dried (MgSO4) and the solvents were removed in vacuo. The residue was purified by distillation in vacuo to give 3-bromo-4-fluorobenzo[b]thiophene (12.5 g) as a pale yellow oil, b.p. 70-85 C. a 0.53 mbar., 310466-38-7

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Reference£º
Patent; Doyle, Kevin James; Kerrigan, Frank; Watts, John Paul; US2003/166628; (2003); A1;,
Benzothiophene – Wikipedia
Benzothiophene | C8H6S – PubChem

 

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310466-38-7, 4-Fluorobenzo[b]thiophene is a benzothiophene compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Preparation of N-t-Butoxycarbonyl-4-(4-fluorobenzo[b]thiophen-2-yl)-4-piperidinol. [0342] Scheme IA, Step A: To a solution of 4- and 6-fluorobenzo[b]thiophene (1.70 g, 11.2 mmol) in dry THF (50 mL) at -78 C. was added 1.6 M n-BuLi in hexanes (9.08 mL, 14.5 mmol). The solution was stirred at -78 C. for 35 min. N-t-butoxycarbonyl-4-piperidone (2.67 g, 15.6 mmol) dissolved in THF (10 mL) was added via a cannula at -78 C. The reaction mixture was kept at -78 C. for 1.5 h, then allowed to warm to room temperature. The reaction was quenched with 150 mL of saturated aqueous NH4Cl solution. The mixture was then extracted (3¡Á300 mL) with EtOAc. The combined organic layers were dried over MgSO4 and filtered. The filtrate was concentrated and purified by medium pressure chromatography (silica gel, 20% EtOAc/hexanes) to give the intermediate title compound as a white foam (0.525 g, 13%). IR (CHCl3) 3350 (br), 1683, 1244 cm-1. Ion Spray MS 352 (M+H)+; 234 (M-(BOC+H20)+; 278 (M-73)+ (base peak); 410 (M+CH3COO-)-, 310466-38-7

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Reference£º
Patent; Hansen, Marvin Martin; He, John Xiaoqiang; Honigschmidt, Nicholas Allan; Koch, Daniel James; Kohn, Todd Jonathan; Rocco, Vincent Patrick; Spinazze, Patrick Gianpietro; Takeuchi, Kumiko; US2004/6229; (2004); A1;,
Benzothiophene – Wikipedia
Benzothiophene | C8H6S – PubChem

 

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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.310466-38-7,4-Fluorobenzo[b]thiophene,as a common compound, the synthetic route is as follows.

EXAMPLE 56 [0349] Preparation of (2S)-3-[(2R,4R)-4-(4-Fluorobenzo[b]thiophen-2-yl)-2-methylpiperidinyl]-1-(1H-indol-4-yl)oxy-2-propanol oxalate. [CHEMMOL-00107] [0350] Preparation of N-t-Butoxycarbonyl-4-(4-fluorobenzo[b]thiophen-2-yl)-2-methyl-4-piperidinol. [0351] Scheme IA, Step A: To a solution of 4- and 6-fluorobenzo[b]thiophene (12.4 g, 81.7 mmol, prepared in example 55) in dry THF (415 mL) at -78 C. was added 1.6 M n-BuLi in hexanes (56.4 mL, 90.2 mmol). The solution was stirred at -78 C. for 1.5 h. N-t-butoxycarbonyl-2-methyl-4-piperidone (15.7 g, 73.5 mmol) dissolved in THF (40 mL) was added via a cannula at -78 C. The reaction mixture was stirred at -78 C. for 4 h. The reaction was then quenched with 300 mL of saturated aqueous NH4Cl solution. The mixture was extracted (2¡Á500 mL) with EtOAc. The combined organic layers were then dried over MgSO4 and filtered. The filtrate was concentrated and purified by medium pressure chromatography (15% EtOAc/hexanes) to give the title compound as a white foam (3.66 g, 14%). 1HNMR (CDCl3) 7.54 (d, J=8.8 Hz, 1H), 7.25 (s, 1H), 7.22 (m, 1H), 6.96 (dd, J=9.0, 8.1, 1H), 4.31 (distt, 1H), 3.85 (m, 1H), 3.18 (dt, J=13.0, 2.9 Hz, 1H), 2.02-1.82 (m, 1H), 1.64 (dd, J=14.2, 6.8, 1H), 1.54-1.44 (m, 11H), 1.28 (d, J=6.8 Hz, 3H), 310466-38-7

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Reference£º
Patent; Hansen, Marvin Martin; He, John Xiaoqiang; Honigschmidt, Nicholas Allan; Koch, Daniel James; Kohn, Todd Jonathan; Rocco, Vincent Patrick; Spinazze, Patrick Gianpietro; Takeuchi, Kumiko; US2004/6229; (2004); A1;,
Benzothiophene – Wikipedia
Benzothiophene | C8H6S – PubChem

 

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310466-38-7, 4-Fluorobenzo[b]thiophene is a benzothiophene compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Scheme IA, step A: To a solution of 4- and 6-fluorobenzo[b]thiophene (1.70 g, 11.2 mmol) in dry THF (50 mL) at -78 C. was added 1.6 M n-BuLi in hexanes (9.08 mL, 14.5 mmol). The solution was stirred at -78 C. for 35 min. N-t-Butoxycarbonyl-4-piperidone (2.67 g, 15.6 mmol) dissolved in THF (10 mL) was added via a cannula at -78 C. The reaction mixture was kept at -78 C. for 1.5 h then allowed to warm to room temperature. The reaction was then quenched with 150 mL of saturated aqueous NH4Cl solution. The mixture was extracted (3¡Á300 mL) with EtOAc. The combined organic layers were dried over MgSO4 and filtered. The filtrate was concentrated and purified by medium pressure chromatography (silica gel, 20% EtOAc/hexanes) to give the intermediate title compound as a white foam (2.24 g, 57%). mp 48-51 C. IR (CHCl3) 3350 (br), 1682,1250 cm-1. Ion Spray MS 352 (M+H)+; 234 (M-(BOC+H2O)+; 278 (M-73)+ (base peak); 410 (M+CH3COO-)-.

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Reference£º
Patent; He, John Xiaoqiang; Honigschmidt, Nicholas Allan; Kohn, Todd Jonathan; Rocco, Vincent Patrick; Spinazze, Patrick Gianpietro; Takeuchi, Kumiko; US2003/232833; (2003); A1;,
Benzothiophene – Wikipedia
Benzothiophene | C8H6S – PubChem

 

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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.310466-38-7,4-Fluorobenzo[b]thiophene,as a common compound, the synthetic route is as follows.

General procedure: A solution of 2,6-difluorobenzaldehyde 7 (1.0g, 7.0mmol) and potassium carbonate (1.45g, 10.5mmol) in DMF (25mL) at 0C was added slowly with methyl thioglycolate (0.7mL, 7.7mmol) and the mixture was stirred at the same temperature for 30min. The reaction mixture was stirred at room temperature for 14h and then at 60C for 6h. Solvent was removed and the resulting residue was diluted with ethyl acetate (60mL) followed by washed with water (20mL). The organic layer was dried over Na2SO4, filtered, and concentrated to obtain a crude compound. The above crude compound (500mg, 2.38mmol) and potassium hydroxide (400mg, 7.14mmol) were taken into a mixture of EtOH/ water (12/2mL) and heated to reflux for 2h. The reaction mixture was cooled to room temperature and concentrated. The resulting residue was diluted with water (20mL), acidified with 6N HCl and extracted with ethyl acetate (60mL). The organic layer was dried over Na2SO4, filtered, and concentrated to afford colorless crystals. The resulting colorless crystals (1.0g, 5.1mmol) were mixed together with powdered copper (97mg, 1.53mmol) in quinoline (10mL) and heated at 185C for 2h. The reaction mixture was cooled to room temperature and diluted with ethyl acetate (60mL) and 2N HCl (20mL). The mixture was filtered and washed with ethyl acetate (50mL). The organic layer was dried over Na2SO4, filtered, and concentrated. The resulting crude product was purified by column chromatography using hexane to give colorless oil. To a solution of the above compound (1.0g, 6.57mmol) in dry THF (13mL) was added a 1.6M solution of n-BuLi in hexane (4.2mL, 6.57mmol) drop wise at-78C. The reaction mixture was stirred at same temperature for 30min and was added tri-n-butyltin chloride (1.79mL, 6.57mmol). The resulting solution was stirred for 1h at-78C and then at room temperature for another 1h. The reaction mixture was concentrated under reduced pressure and the resulting residue was diluted with ethyl acetate (60mL), washed with aqueous KF (2¡Á20mL) and with water (2¡Á20mL). The combined organic layers ware dried over MgSO4 and concentrated to obtain a crude product. A solution of the above crude compound (1.0g, 2.27mmol) and 2-bromopyridine (360mg, 2.27mmol) in toluene (22mL) was added with Pd(PPh3)4 (131mg, 0.114mmol). The reaction mixture was degassed thoroughly with nitrogen and stirred at 110C for 8h. After cooling to room temperature, the mixture was concentrated under reduced pressure. The obtained crude product was diluted with ethyl acetate, filtered through Celite, and washed with aqueous KF (2¡Á15mL) followed by brine (15mL) and water (15mL). The organic layer was dried over MgSO4, filtered, and concentrated to afford a crude product which was purified by column chromatography using ethyl acetate/hexane (1:9) to afford the pure compound 8 as a white solid (260mg 40%).

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Reference£º
Article; Li, Chung-Yen; Su, Chaochin; Wang, Hsiou-Hsuan; Kumaresan, Prabakaran; Hsu, Chia-Hsuan; Lee, I-Ting; Chang, Wei-Chun; Tingare, Yogesh S.; Li, Ting-Yu; Lin, Chia-Feng; Li, Wen-Ren; Dyes and Pigments; vol. 100; 1; (2014); p. 57 – 65;,
Benzothiophene – Wikipedia
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