Day: September 3, 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.822-82-2,Isothiazole-4-carboxylic acid,as a common compound, the synthetic route is as follows.

822-82-2, solution of 1 ,2-thiazole-4-carboxylic acid (36 mg, 0.28 mmol) and HATU (105 mg, 0,28 mmol) in DMA (1 mL) was added to a mixture of N-{4-[4-oxo-3-(phenylamino)-4,5,6,7- tetrahydro-1 H-pyrrolo[2,3-c]pyridin-2-yl]pyridin-2-yl}acetamide (24; 50 mg, 0.14 mmol) and DIPEA (48 pL, 0.28 mmol) in DMA (1 mL) and stirred for 16 h at 50X. The mixture was concentrated and purified by preparative HPLC (basic method) to give the title compound (37 mg, 54%). 1H-NMR (400 MHz, DMSO-d6), delta [ppm]= 2.08 (3H), 4.14+4.34 (2H), 4.90+5.08 (2H), 6.58 (2H), 6.60 (1 H), 7.03 (2H), 7.21 (1 H), 7.45 (1 H), 8.13 (1 H), 8.23+8.29 (1 H), 8.71 +8.80 (1 H), 9.35+9.45 (1 H), 10.41 (1 H), 12.07+12.36 (1 H)

822-82-2 Isothiazole-4-carboxylic acid 12430656, aisothiazole compound, is more and more widely used in various.

Reference£º
Patent; BAYER PHARMA AKTIENGESELLSCHAFT; GRAHAM, Keith; KLAR, Ulrich; BRIEM, Hans; SIEMEISTER, Gerhard; MOeNNING, Ursula; VON NUSSBAUM, Franz; (332 pag.)WO2017/102649; (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.

0.75 mmol of 3,4-dichloroisothiazole-5-carboxylic acid I-1 was added to a 100 ml two-neck round bottom flask.1-(3-Methylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDCI) was 0.9 mmol, 1-hydroxybenzotriazole (HOBT) was 0.77 mmol, dissolved in dichloro Methane (25 mL) was stirred in an ice bath for 15 minutes.A solution of the amine II-1 in dichloromethane (25 mL) was added to the reaction mixture, then 0.90 mmol of Et3N was added, and the reaction mixture was stirred at room temperature for 16 hours.After the reaction was completed, the organic layer was washed with water (2¡Á30 mL) and brine (40 mL).The organic layer was dried over MgSO 4 and concentrated under reduced vacuo.The residue is purified by silica gel column chromatography on 100~200 mesh to give compound III-1.The eluent was petroleum ether: ethyl acetate at 60 to 90 C, and the volume ratio was 5:1, and the yield was 56%; the amount of the compound III-1 prepared and the volume of the reaction vessel were expanded or reduced in a corresponding ratio., 18480-53-0

18480-53-0 3,4-Dichloroisothiazole-5-carboxylic acid 49837, aisothiazole compound, is more and more widely used in various.

Reference£º
Patent; Nankai University; Fan Zhijin; Yang Dongyan; Li Zhengming; Zhu Yilin; Zhou Jinghui; Guo Xiaofeng; Zhang Nailou; Wu Qifan; Yu Bin; Zhou Shuang; (19 pag.)CN110041324; (2019); A;,
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

n-Butyllithium (2.5 M solution in hexanes, 10.5 mL, 26.2 mmol) was added to a-78 00 solution of diisopropylamine (3.68 mL, 26.3 mmol) in tetrahydrofuran (80 mL).After 30 minutes, a solution of 4-bromo-1 ,2-thiazole (3.70 g, 22.5 mmol) intetrahydrofuran (20 mL) was added drop-wise, and stirring was continued at -78 00 for 30 minutes, whereupon methyl carbonocyanidate (99%, 2.15 mL, 26.8 mmol) was added. After an additional 30 minutes at -78 00 the reaction mixture was quenched via addition of saturated aqueous ammonium chloride solution, and the resulting mixturewas warmed to room temperature. After dilution with water, it was extracted with ethyl acetate; the combined organic layers were washed with saturated aqueous sodium chloride solution, dried over magnesium sulfate, filtered, and concentrated in vacuo. Purification via silica gel chromatography (Eluent: 5% ethyl acetate in heptane) provided the product as a white solid. Yield: 4.0 g, 18 mmol, 80%. 1H NMR (400 MHz, ODd3) oe8.43 (5, 1H), 3.97 (5, 3H)., 24340-77-0

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

Reference£º
Patent; PFIZER INC.; GRAY, David Lawrence Firman; ZHANG, Lei; DAVOREN, Jennifer Elizabeth; DOUNAY, Amy Beth; EFREMOV, Ivan Viktorovich; MENTE, Scot Richard; SUBRAMANYAM, Chakrapani; WO2015/162515; (2015); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

822-82-2, Isothiazole-4-carboxylic acid is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

822-82-2, To a solution of l-[4-[ethyl(tetrahydropyran-4-yl)amino]-5-oxido-6,7-dihydro- thieno[3,2-d]pyrinnidin-5-iunn-2-yl]azetidin-3-ol (5.0 mg, 14 muiotatauiotaomicronIota) in DCE (0.2 mL) was added solutions of 4-isothiazolecarboxylic acid (2.7 mg in 0.2 mL DCE, 21 muiotatauiotaomicronIota), DMAP (0.52 mg in 0.1 mL DCE, 4.3 muiotatauiotaomicronIota) and EDAC (4.1 mg in 0.1 mL DCE, 21 muiotatauiotaomicronIota). The mixture was shaken at 50 C for 20 minutes before it was concentrated in vacuo. Prep HPLC purification (basic) afforded the title compound as colorless oil. 1H NMR (DMSO-d6) delta: 9.81 (s, 1H), 9.00 (s, 1H), 5.52 – 5.45 (m, 1H), 4.84 – 4.68 (m, 1H), 4.53 – 4.40 (m, 2H), 4.13 (dd, 2H), 3.97 (td, J = 11.2, 4.3 Hz, 2H), 3.71 – 3.56 (m, 2H), 3.51 – 3.43 (m, 1H), 3.43 – 3.34 (m, 2H), 3.25 – 3.18 (m, 1H), 3.07 – 2.97 (m, 2H), 1.95 – 1.82 (m, 2H), 1.75 (d, J = 12.3 Hz, 1H), 1.62 (d, 1H), 1.19 (t, J = 6.9 Hz, 3H). HPLC-Retention time (XE Metode 7 CM) : 1.95 minutes. Detected “M + l”-mass: 464.15.

822-82-2 Isothiazole-4-carboxylic acid 12430656, aisothiazole compound, is more and more widely used in various.

Reference£º
Patent; LEO PHARMA A/S; LARSEN, Jens; (110 pag.)WO2019/57806; (2019); 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.677304-75-5,6-Bromobenzo[d]isothiazole-3-carboxylic acid,as a common compound, the synthetic route is as follows.

677304-75-5, Step 5[00200] Sulfuryl dichloride (86.7 mg, 728 mumol) was added to a solution of 6- bromobenzo[d]-isothiazole-3-carboxylic acid (188 mg, 728 mumol). The reaction mixture was stirred for 30 min before removing the volatiles by rotovap. The residue was taken up in CH2Cl2 (0.587 ml) and a solution of 2-propylamine (62.5 muL, 728 mumol) and triethylamine (101 mul, 728 mumol) in CH2Cl2 (1.2 ml) was added. The reaction mixture was stirred at room temperature until LCMS analysis indicated complete conversion to the desired product. The reaction mixture was diluted with distilled water and ethyl acetate. The layers were separated and the aqueous was extracted with ethyl acetate. The combined organics were washed with brine and dried over Na2SO4, filtered and concentrated to give 6-bromo-N- isopropylbenzo[d]isothiazole-3-carboxamide.

As the paragraph descriping shows that 677304-75-5 is playing an increasingly important role.

Reference£º
Patent; AMGEN INC.; MEMORY PHARMACEUTICALS CORPORTION; WO2007/98169; (2007); 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.288-16-4,Isothiazole,as a common compound, the synthetic route is as follows.

Under nitrogen protection, compound 1 was added(20 g, 0.235 mol) was added to dry 100 ml of ether and stirred and dissolvedTemperature below 0 ,To this was added n-butyllithium (0.24 mol), and the mixture was kept at 0 C or less during the dropping,After the dropwise addition, the incubation reaction was carried out until no compound 1 was added.To the reaction solution was added bromine (0.5 mol)The reaction mixture was kept at 0 C or lower, and the mixture was slowly added to the room temperature after completion of the dropwise addition. After stirring for half an hour, the reaction was quenched by adding hydrochloric acid solution (2N, 500 ml) thereto.And the aqueous phase was extracted with ether (200 ml * 3) and discarded. The organic phase was combined and washed with sodium dithionite solution(100 ml * 2), dried over anhydrous sodium sulfate, filtered and concentrated to dryness to give compound 2 as a yellow oil.

288-16-4, The synthetic route of 288-16-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Tianjin Jinyao Group Co., Ltd.; Li Jing; He Guangjie; Yang Xinyi; Wang Shuli; Chen Liying; Hu Xiaoyun; Sun Liang; (37 pag.)CN106890179; (2017); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

87691-88-1,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.

Examples 1. Preparation of ZPR in n-BuOH with 0.9 mol NaI. In a three necked flask was charged n-BuOH (50 ml) and 1, 2-Benzisothiazole-3- piperazinyl hydrochloride (BITP HC1) (5.6g, 0.022 mol), and the obtained slurry was heated at 100C. To the slurry, Na2CO3 (11.6 g), NaI (3g) and 5- (2-chloroethyl)-6- chloro-1, 3-dihydro-indole-2 (2H)-one (CEI) (7. 5g, 0.032 mol) were added at 110C. The heating was maintained for 8. 5h. After cooling the reaction product was filtrated, washed with hexane and water, and dried at 60 C. The dried product weights 8.12g and has an HPLC purity 92.7%.

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

Reference£º
Patent; TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.; WO2005/40160; (2005); A2;,
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.

EXAMPLE 6 Synthesis of potassium 3,4-dichloroisothiazole-5-carboxylate (Compound No. 7) Potassium hydroxide (0.27 g) dissolved in 3 ml of water was added to a solution of 3,4-dichloroisothiazole-5-carboxylic acid (0.95 g) in 4 ml of ethanol. The solvent was distilled off under reduced pressure. The crystals thus obtained were washed with a small quantity of ethanol.

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

Reference£º
Patent; Mitsui Toatsu Chemicals, Incorporated; US5240951; (1993); 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

87691-88-1, (iii) Preparation of 5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-2H-indol-2-one : Charge 1.0 litre demin water, 100 gm of step (ii) product, 122.4 gm 3-(1-piperazinyl)-1,2-benzisothiazole HCl] and 138.2 gm of sodium carbonate into a 3 litre three neck flask at 25 to 30C. Stir for 15 mins and heat to reflux temperature 95 to 100C. Maintain at reflux temperature for 15 hrs. Cool the reaction mixture to 45-50C. Add 1.0 lt of demin water into the reaction mixture and stir for 30 mins. Filter at 45 to 50C and wash with demin water. Suck dry for 30 mins to yield crude product. Charge 2 lt of demin water and above crude product and heat the mixture gradually to 45 to 50C and stir for 30 mins. Filter the product at 45 to 50C and wash with demin water. Suck dry the product for 30 mins. Charge 2.0 lt of demin water and 300 gm of crude product into a 1.0 litre three neck flask at 25 to 30C and heat the mixture gradually to 45 to 50C. Stir for 30 mins. Filter the product at 45 to 50C and wash with demin water till about neutral pH (6.5 to 7.0). Suck dry the product for 30 mins to get wet crude base [5-[2- [4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-2H-indol-2-one. Add 300 gms of wet crude base and 1.0 lt of isopropanol at 25 to 30C. Warm the reaction mixture to 50 to [55C] and stir for 1.0 hr. Cool the reaction mixture gradually to 10 to 15C and stir for 30 mins. Filter the product and wash with chilled isopropanol. Suck dry for 30 mins. Charge 300 gm of wet crude base and 6 lt of tetrahydrofuran (THF). Heat the reaction mixture gradually to reflux temperature 65- 70C. Reflux till clear solution. Cool to 50 to 55C and add charcoal and stir for 30 min at 50 to 55C. Filter the charcoal and wash with hot THF. Distill out THF at 50 to 55C under vacuum till residual volume is 1 lt and cool the reaction mixture gradually to 5 to 10C and stir for 1 hr. Filter the product and wash with chilled THF. Suck dry the product for 30 mins. Dry the product at 60 to 65C.

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

Reference£º
Patent; SUN PHARMACEUTICAL INDUSTRIES LIMITED; WO2003/99198; (2003); A2;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com