Day: August 20, 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.87691-88-1,3-Piperazinobenzisothiazole hydrochloride,as a common compound, the synthetic route is as follows.

EXAMPLE 79 3-(4-(1-(1,2-Benzisothiazol-3-yl)-4-piperazinyl)butyl)-2-methyl-1-thia-3-azaspiro[4.4]nonan-4-one hydrochloride A mixture of 3-(4-bromobutyl)-2-methyl-1-thia-3-azaspiro[4.4]nonan-4-one (3.84 g), 1-(1,2-benzisothiazol-3-yl)piperazine hydrochloride (3.49 g), K2 CO3 (5.90 g) and NaI (280 mg) in acetonitrile (215 ml) was heated at between 65-80 C. for 16.5 hours and the product was processed in substantially the same manner as in Example 10 to afford 2.86 g of crystals, m.p. 210-215 C. ANALYSIS: Calculated for C23 H32 N4 OS2 ¡¤HCl: 57.42%C; 6.91%H; 11.64%N; 7.37%Cl. Found: 57.21%C; 6.87%H; 11.63%N; 7.03%Cl.

As the paragraph descriping shows that 87691-88-1 is playing an increasingly important role.

Reference£º
Patent; Hoechst-Roussel Pharmaceuticals Incorporated; US5229388; (1993); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

288-16-4, Isothiazole is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 26 N-[alpha-(5-isothiazolyl)benzyl]-4-pyridinamine The title compound is prepared in a similar manner to Examples 5, 6 and 7 by reacting 5-isothiazolyl lithium (formed from isothiazole and butyl lithium) with 4-benzylideneaminopyridine.

288-16-4 Isothiazole 67515, aisothiazole compound, is more and more widely used in various.

Reference£º
Patent; John Wyeth & Brother Limited; US4180670; (1979); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

18480-53-0, 3,4-Dichloroisothiazole-5-carboxylic acid is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a suspension of 3,4-dichloroisothiazole-5-carboxylic acid (0.15 g, 0.76 mmol) in oxalyl chloride (2 mL) was added a catalytic amount of dimethylformamide (2 drops) and the mixture was heated to 80¡ã C. and stirred for 2 h. The excess oxalyl chloride was removed on the rotary evaporator. Meanwhile, 5-fluoro-2-(4-fluorobenzyloxy)-pyrimidin-4-ylamine (0.17 g, 0.68 mmol) was dissolved in THF (1 mL), treated with LiHMDS (1M in THF, 0.76 mL, 0.76 mmol) and stirred for 10 min. The freshly prepared 3,4-dichlorothiazole-5-carbonyl chloride*, dissolved in THF (1 mL), was added and the reaction was capped and stirred for 12 h. The reaction was diluted with water and the target compound was extracted with CH2Cl2 (3.x.5 mL). The combined extracts were dried over MgSO4 and then evaporated under reduced pressure. The mixture was eluted with CH2Cl2 through an anionic-exchange solid phase extraction column and then further purified by reverse-phase chromatography to give 3,4-dichloroisothiazole-5-carboxylic acid [5-fluoro-2-(4-fluorobenzyloxy)pyrimidin-4-yl]amide (0.035 g, 12percent) as a tan solid: mp 87-90¡ã C.; 1H NMR (400 MHz, DMSO-d6) delta 11.78 (s, 1H), 8.67 (s, 1H), 7.51-7.48 (m, 2H), 7.24-7.19 (m, 2H), 5.25 (s, 2H); MS (ESI) m/z 417 (M+H)+, 415 (M-H)-. *Nagata, T.; Kogure, A.; Yonekura, N.; Hanai, R.; Kaneko, I.; Nakano, Y. JP 2007211002 A

The synthetic route of 18480-53-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; DOW AGROSCIENCES LLC; US2009/203647; (2009); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

936-16-3, 2,3-Dihydrobenzo[d]isothiazole 1,1-dioxide is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 2.To a solution of 1 (97.0 mg, 0.57 mmol) in DMF (4 mL) was added NaH (13.9 mg, 0.58 mmol) at 0¡ãC. The mixture was stirred at 0¡ãC for 30 minutes. Dichloropyrimidine 2 (100 mg, 0.48 mmol, 1.0 eq) was added, the solution was allowed to warm to 15¡ãC and stirred for 15 hours. The resulting mixture was poured into ice water (w/w = 1/1, 20 mL) and stirred for 10 minutes. The aqueous phase was extracted with EtOAc (30 mL) and the combined organic phase was washed with brine (20 mL), dried with anhydrous Na2S04, filtered, and concentrated in vacuo to afford 3 (120 mg, 72percent).

936-16-3 2,3-Dihydrobenzo[d]isothiazole 1,1-dioxide 13638, aisothiazole compound, is more and more widely used in various.

Reference£º
Patent; NUMERATE, INC.; RAIMUNDO, Brian; KOLTUN, Elena S.; GRIFFIN, John; STANGELAND, Eric; (93 pag.)WO2018/49324; (2018); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.24340-77-0,4-Bromoisothiazole,as a common compound, the synthetic route is as follows.

To a reaction flask were added compound 22 (100 mg, 0.195 mmol), 4-bromoisothiazole (50 mg, 0.293 mmol), Pd(dppf)Cl2 (5 mg, 0.006 mmol) and sodium carbonate (60 mg, 0.558 mmol), 5 mL glycol dimethyl ether and 0.9 mL water were added, bubbled with nitrogen gas for 10 minutes, and the reaction was heated to 100 C in microwave and reacted for half an hour. After TLC detected the reaction was complete, the reaction was concentrated, purified by silica gel column chromatography to afford 42 mg of a product, yield: 46%. LC-MS(APCI): m/z = 469.5 (M+1)+. 1H NMR (400 MHz, CDCl3) delta 8.69 (d, J = 2.4 Hz, 1H), 8.58 (d, J = 9.6 Hz, 2H), 7.94 (d, J = 2.4 Hz, 1H), 7.74 (s, 1H), 7.67 (d, J = 9.0 Hz, 2H), 7.23 (s, 1H), 5.21 (d, J = 52.0 Hz, 1H), 3.56 (d, J = 3.1 Hz, 1H), 3.52 – 3.44 (m, 2H), 3.30 (t, J = 9.7 Hz, 1H), 2.26 – 2.19 (m, 1H), 2.03 – 1.97 (m, 1H).

24340-77-0 4-Bromoisothiazole 5200358, aisothiazole compound, is more and more widely used in various.

Reference£º
Patent; Shenzhen Targetrx, Inc.; WANG, Yihan; ZHAO, Jiuyang; AL, Yixin; (51 pag.)EP3553057; (2019); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

24340-77-0, 4-Bromoisothiazole is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: General Procedure E: Preparation of Coupled Aryl and Heteroaryl Groups Using Buchwald Catalyzed Coupling Conditions Between an Organohalide in the Presence of a Tin Reagent (0331) [00219] A solution of organobromide (1.0 equivalent), organochloride (1.0 equivalent), hexabutylditin (1.0 equivalent) and Pd(dppf)Cl2?DCM (10 mol%) in anhydrous 1,4-dioxane (10 mL/mmol) was stirred at 100 oC under N2 overnight, then cooled and quenched with water (20 mL/mmol). The resulting mixture was extracted with EtOAc (20 mL/mmol x 3), the organic phases were separated and dried over anhydrous Na2SO4 and filtered. The filtrate was concentrated in vacuo, and the resulting residue was purified by silica gel column (0332) chromatography or preparative-TLC to afford the coupled ring system.

The synthetic route of 24340-77-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; LYSOSOMAL THERAPEUTICS INC.; SKERLJ, Renato, T.; BOURQUE, Elyse Marie Josee; LANSBURY, Peter, T.; GREENLEE, William, J.; GOOD, Andrew, C.; (309 pag.)WO2017/176961; (2017); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.18480-53-0,3,4-Dichloroisothiazole-5-carboxylic acid,as a common compound, the synthetic route is as follows.

3,4-Dichloroisothiazol-5-carboxylic acid (0.235 g, 1.2 mmol), dichloromethane (6 ml), N,N-dimethylformamide (2 drops) were added dropwise to the reaction flask. Add oxalyl chloride (1 g, 8 mmol),The reaction solution was stirred at room temperature for 4 hours.The solvent was then evaporated to give 3,4-dichloroisothiazol-5-carbonyl chloride, which was dissolved in dichloromethane (2 mL).Then 4-fluoro-2-(2-pentyloxy)aniline (0.197 g, 1 mmol) was added to the reaction flask and triethylamine (0.13 mL) was added.Further, a 3,4-dichloroisothiazol-5-formyl chloride solution was added dropwise to the reaction flask, and the mixture was stirred at room temperature for 16 hours.Then after monitoring the reaction by thin layer chromatography,Water was added to the reaction mixture, and the mixture was extracted with ethyl acetate.The organic layer was washed with saturated brine.After drying over anhydrous sodium sulfate, it was concentrated under reduced pressure.The residue was purified by column chromatography (eluent: petroleum ether: ethyl acetate = 20:1).Obtained a fresh yellow solid of 0.236 g.The yield was 62.76percent.

As the paragraph descriping shows that 18480-53-0 is playing an increasingly important role.

Reference£º
Patent; Shanghai Taihe International Trade Co., Ltd.; Ma Wenjing; Lv Liang; Li Hongwei; Hou Shuang; Du Yonglei; Liu Jiyong; (31 pag.)CN108383791; (2018); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

87691-88-1, 3-Piperazinobenzisothiazole hydrochloride is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 59; (R)(-)-N-{5-[2-(4-BENZO[D]ISOTHIAZOL-3-YL-PIPERAZIN-1-YL)- ETHYL1-INDAN-2-YLl-ACETAMIDE; A slurry of (R)-N- [5- (2-Chloro-ethyl)-indan-2-yl]-acetamide (2. 00g, 8. 41mmole), Na2CO3(1. 5eq) and 3-Piperazin-1-yl-benzo [d] isothiazole hydrochloride (2. 0eq) in H20 (20moi) was reacted under microwave assistance using a CEM MARS-5 microwave reactor to 175C for 10min. Upon cooling, the reaction was diluted with EtOAc (250moi), H20 (100mol) and the layers separated. The aqueous layer was extracted with EtOAc (2x 50ml). The organics were dried (MgSO4), concentrated, and the residue purified by chromatography (EtOAc) to give (R) (-)-N- {5- [2- (4- Benzo [d] isothiazol-3-yl-piperazin-1-yl)-ethyl]-indan-2-yl}-acetamide (2. 92g, 6. 94mmole) in 100% purity 254 nm; LCMS (APCI) 474 [M+H] +. [a] D25- 3. 6 (c 5.5, CHCl3). 1 H NMR (400 MHz, CHLOROFORM-D) 8 ppm 1.94 (s, 3 H) 2.65-2. 71 (m, 2 H) 2.73-2. 80 (m, 6 H) 2.81-2. 87 (m, 2 H) 3.28 (ddd, J=16. 04,6. 10,5. 92 Hz, 2 H) 3.57-3. 62 (m, 4 H) 4.69-4. 76 (m, 1 H) 5.70 (d, J=7.08 Hz, 1 H) 7.06 (d, J=7.81 Hz, 1 H) 7.11 (s, 1 H) 7.16 (d, J=7.56 Hz, 1 H) 7.35 (ddd, J=8.17, 7.08, 1.10 Hz, 1 H) 7.46 (ddd, J=8.11, 7.02, 1.22 Hz, 1 H) 7.81 (dt, J=8.05, 0.85 Hz, 1 H) 7.91 (dt, J=8.30, 0.98 Hz, 1 H).

87691-88-1 3-Piperazinobenzisothiazole hydrochloride 11521711, aisothiazole compound, is more and more widely used in various.

Reference£º
Patent; WARNER-LAMBERT COMPANY LLC?; WO2005/56540; (2005); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

111248-89-6, 1,3-Dihydrobenzo[c]isothiazole 2,2-dioxide is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

4c. 1-Methyl-i ,3-dihydrobenzo[c]isothiazole-2 ,2-dioxide To a suspension of I ,3-dihydrobenzo[c]isothiazole-2,2-dioxide (280 mg,1.655 mmol) and potassium carbonate (229 mg, 1.66 mmol) in DMF (5 mL) was added iodomethane (414 pL, 6.62 mmol). The reaction was stirred for 6 hr at RT andwas then quenched with a sat. NH4CI solution. The reaction mixture was concentratedand purified by column chromatography (CyHex/acetone) to afford the title compound asa white solid (270 mg, 89%). 1H NMR (500 MHz, CDCI3) ppm = 7.37-7.32 (m, 1H), 7.27-7.24 (m, 1H), 7.02 (td, J=7.6, 1.0, IH), 6.73 (d, J8.0, IH), 4.34 (s, 2H), 3.14 (s, 3H); Rt= 2.07 mm (H PLC method F).

The synthetic route of 111248-89-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MERCK PATENT GMBH; CANCER RESEARCH TECHNOLOGY LIMITED; SCHIEMANN, Kai; STIEBER, Frank; CALDERINI, Michel; BLAGG, Julian; MALLINGER, Aurelie; WAALBOER, Dennis; RINK, Christian; CRUMPLER, Simon Ross; (127 pag.)WO2015/144290; (2015); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

18480-53-0, 3,4-Dichloroisothiazole-5-carboxylic acid is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Preparation of the starting material: At room temperature, 146 g (1.23 mol) of thionyl chloride are added dropwise with stirring over a period of 5 minutes to 8.92 g (0.045 mol) of 3,4-dichloro-isothiazole-5-carboxylic acid. 4 drops of dimethylformamide are then added, and the reaction mixture is heated at reflux for one hour. The reaction mixture is subsequently cooled to room temperature and concentrated under reduced pressure. This gives 12.19 g of 3,4-dichloro-isothiazole-5-carbonyl chloride in the form of an orange oil. The compounds of the formula (I) listed in the table below are also prepared by the method given above.

The synthetic route of 18480-53-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Bayer Aktiengesellschaft; US6191155; (2001); B1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com