Heterocyclic Building Blocks-Isothiazole

288-16-4, In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. Isothiazole, cas is 288-16-4,the isothiazole compound, it is a common compound, a new synthetic route is introduced below.

Compound 1 (20 g, 0.235 mol) was added under stirring with nitrogen to dry 100 ml of ether and stirred and dissolvedThe temperature is 0 C or lower, n-butyllithium (0.24 mol) is added dropwise thereto, and the mixture is kept at 0 C or lower during the dropwise addition.Temperature reaction until no compound 1.To the reaction solution was added dropwise bromine (0.5 mol), and the mixture was kept below 0 C during the dropwise addition, and the mixture was gradually raised toAfter 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.

Chemical properties determine the actual use. Each compound has specific chemical properties and uses. We look forward to more synthetic routes in the future to expand reaction routes of Isothiazole, 288-16-4

Reference£º
Patent; Tianjin Jinyao Group Co., Ltd.; Li Jing; He Guangjie; Yang Xinyi; Wang Shuli; Chen Liying; Hu Xiaoyun; Sun Liang; (38 pag.)CN106890180; (2017); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

936-16-3, In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 2,3-Dihydrobenzo[d]isothiazole 1,1-dioxide, cas is 936-16-3,the isothiazole compound, it is a common compound, a new synthetic route is introduced below.

Example 27. 4-(1,1-Dioxido-1,2-benzisothiazol-2(3H)-yl)-2-piperazin-1-ylquinazoline. 2,4-Dichloroquinazoline (60 mg, 0.30 mmol), 2,3-dihydro-l,2-benzisothiazole 1,1-dioxide (50 mg, 0.30 mmol) and sodium hydride (11 mg, 0.45 mmol) were dissolved in anhydrous DMF (2 ml). The mixture was heated at 60¡ã C under nitrogen atmosphere for 10 min. Piperazine (52 mg, 0.60 mmol) was added and the heating was continued for 10 minutes. 5 The reaction mixture was diluted with water (0.5 ml), filtered and purified by preparative HPLC to give the acetate of the title compound as a solid (36 mg, 27 percent). 1H NMR (400 MHz, MeOD-d4) delta ppm 8.49 (1 H3 d) 7.58 – 7.87 (6 H, m) 730 – 7.38 (1 H, m) 5.58 (2 H, s) 4.03 – 4.16 (4 H3 m) 3.15 – 3.26 (4 H3 m); ESI-MS m/z M+H+ 382.

The chemical industry reduces the impact on the environment during synthesis,936-16-3,2,3-Dihydrobenzo[d]isothiazole 1,1-dioxide,I believe this compound will play a more active role in future production and life.

Reference£º
Patent; ASTRAZENECA AB; WO2007/108743; (2007); A2;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

As a common heterocyclic compound, it belongs to isothiazole compound, name is 3-Piperazinobenzisothiazole hydrochloride, and cas is 87691-88-1, its synthesis route is as follows.

EXAMPLE 75 3-[4-[1-(1,2-Benzisothiazol-3-yl)-4-piperazinyl]-butyl]-1-thia-3-azaspiro[4.4]nonan-4-one A mixture of 3-(4-bromobutyl)-1-thia-3-azaspiro[4.4]-nonan-4-one (4.50 g), 1-(1,2-benzisothiazol-3-yl)piperazine hydrochloride (4.33 g), K2 CO3 (7.45 g) and NaI (560 mg), in acetonitrile (220 ml) was heated at 65 C. for 14.5 hours and the product was processed in substantially the same manner as in Example 10 to afford 2.25 g of crystals, m.p. 200-203 C. ANALYSIS: Calculated for C22 H30 N4 OS2 *HCl: 56.57%C; 6.69%H; 11.99%N; 7.59%Cl. Found: 56.15%C; 6.75%H; 12.11%N; 7.88%Cl.

87691-88-1, In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles.,87691-88-1 ,3-Piperazinobenzisothiazole hydrochloride, other downstream synthetic routes, hurry up and to see

Reference£º
Patent; Hoechst-Roussel Pharmaceuticals Inc.; US4933453; (1990); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

288-16-4, In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. Isothiazole, cas is 288-16-4,the isothiazole compound, it is a common compound, a new synthetic route is introduced below.

a) 5-Isothiazolecarboxylic acid was prepared from isothiazole, n-BuLi and dry ice according to the method of step a of Example 258.

Chemical properties determine the actual use. Each compound has specific chemical properties and uses. We look forward to more synthetic routes in the future to expand reaction routes of Isothiazole, 288-16-4

Reference£º
Patent; Monsanto Company; US5498630; (1996); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

87691-88-1, In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 3-Piperazinobenzisothiazole hydrochloride, cas is 87691-88-1,the isothiazole compound, it is a common compound, a new synthetic route is introduced below.

N- [4- (2-CHLORO-ETHYL)-2-METHYL-PHENYL]-N-METHYL-ACETAMIDE (0.300 g, 1. 153 mmol), 3-PIPERAZIN-1-YL-BENZO [d] isothiazole hydrochloride (0.442 g, 1.729 MMOL), potassium carbonate (0.237 g, 1.729 MMOL), and potassium iodide (0.173 g, 1.153 MMOL) in ACETONITRILE (3.5 mL) was subjected to 150 C for 30 min. under microwave assistance using a Smith Personal Chemistry microwave. The reaction was diluted with H20 (50 mL) and CH2CI2 (100 mL). The layers were separated and the organics washed with 1 N HCI (2x 25 mL). The aqueous layer was made basic and extracted with CH2CI2 (3X50 mL). The organics were dried (MGS04), and concentrated to a solid residue. The residue was subjected to chromatography (MEOH : CH2CI2 1 : 19) and collected as an amorphous residue and taken up in 1,4-dioxane and subjected to HCI gas for 10 min. The resulting solid was collected by filtration and dried at 50 C under high vacuum overnight (0.770 g). 100% purity at 254nm; LCMS (APCI) : 409.2 [M+H] +.

The chemical industry reduces the impact on the environment during synthesis,87691-88-1,3-Piperazinobenzisothiazole hydrochloride,I believe this compound will play a more active role in future production and life.

Reference£º
Patent; WARNER-LAMBERT COMPANY LLC; WO2004/41793; (2004); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

As a common heterocyclic compound, it belongs to isothiazole compound, name is 2,3-Dihydrobenzo[d]isothiazole 1,1-dioxide, and cas is 936-16-3, its synthesis route is as follows.

Step 2. To a solution of 8 (150 mg, 0.54 mmol) and 1 (92 mg, 0.54 mmol) in anhydrous DMF (4 mL) was added cesium carbonate (353 mg, 1.08 mmol), and the resulting mixture was stirred at 40¡ãC for 2 hours. Upon completion, the reaction mixture was poured into water (10 mL) and extracted with ethyl acetate (60 mL). The combined organic layer was washed with saturated brine, dried over anhydrous sodium sulfate, filtered and concentrated under reduced pressure. Purification by prep-HPLC (0.04percentHCl/CH3CN/H2O system) resulted in Compound 77 (3.9 mg, 9.0percent) as a white solid. 1H NMR (DMSO-d6, 400MHz) delta 8.78 (d, 1H), 8.61 (d, 1H), 8.10-8.03 (m, 2H), 7.84 (d, 1H), 7.76-7.71 (m, 3H), 6.99 (s, 1H), 5.14 (s, 2H), 2.40 (s, 3H); LCMS (ESI): m/z 355.0 (M+H).

936-16-3, In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles.,936-16-3 ,2,3-Dihydrobenzo[d]isothiazole 1,1-dioxide, other downstream synthetic routes, hurry up and to see

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

Name is 3-Piperazinobenzisothiazole hydrochloride, as a common heterocyclic compound, it belongs to isothiazole compound, and cas is 87691-88-1, its synthesis route is as follows.

Example 5Preparation of 5-[2-[4-(l,2-benzisothiazol-3-yl)-l-piperazinyn]ethyl]-6- chloro-l,3-di hydro-2H- indol-2-one:Charge 1.0 litre water, 100 gm of 5-(2-chloroethvl)-6-chlorooxindole product, 122.4 gm 3-(l-piperazinyl)-l,2-benzisothiazole HCI and 138.2 gm of sodium carbonate into a 3 litre three neck flask at 25 to 30 C. Stir for 15 minutes and heat to reflux temperature 95 to 100 C. Maintain at reflux temperature for 15 hrs. Cool the reaction mixture to 45 – 50C. Add 1.0 It of water into the reaction mixture and stir for 30 minutes. Filter at 45 to 50 C and wash with water. Suck dry for 30 minutes to yield crude product. Charge 2 It of water and above crude product and heat the mixture gradually to 45 to 50C and stir for 30 minutes. Filler the product at 45 to 50C and wash with water. Suck dry the product for 30 minutes. Charge 2.0 It of 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 water till about neutral pH (6.5 to 7.0). Suck dry the product for 30 minutes to get wet crude base 5-[2-[4-(l,2-benzisothiazo.-3-yl)-l-piperazinyl]ethylj-6- chloro-i,3-di hydro- 2H- indol-2-one. Add 300.-gms of wet crude base and 1.0 It 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 minutes. Charge 300gm of wet crude base and 6 It 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 55dC. Filter the charcoal and wash with hot THF. Distill out THF at 50 to 55 C under vacuum till residual volume is 1 It 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 minutes. Dry the product at 60 to 65C.

87691-88-1, In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles.,87691-88-1 ,3-Piperazinobenzisothiazole hydrochloride, other downstream synthetic routes, hurry up and to see

Reference£º
Patent; ARCH PHARMALABS LIMITED; GHOGARE, Bhausaheb Nana; DESHPANDE, Uday K.; PAI, Ganesh Gurpur; MANDAL, Arun Kanti; CHARANJIT, Sehgal; NEHA, Dixit Akshaya; WO2012/20424; (2012); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

As a common heterocyclic compound, it belongs to isothiazole compound, name is Benzo[d]isothiazole-3(2H)-thione 1,1-dioxide, and cas is 27148-03-4, its synthesis route is as follows.

A solution of thiosaccharin (tsacH) (0.084 g, 0.425 mmol) in chloroform (10 cm3) was added to a solution of [Pt(kappa2-dppm)2]Cl2 (0.22 g, 0.22 mmol) in chloroform (10 cm3). A few drops of triethylamine were added and the resulting mixture was heated under reflex for 1 h. This produced a yellow solution which was filtered and reduced to half volume. Methanol (2 cm3) was added and the mixture was set aside to evaporate slowly at room temperature. The pale yellow crystalline solid thus formed was filtered off and dried in a vacuum oven (85%). 11: pale yellow solid, 85% yield. 1H NMR: delta 7.57 (d, J 7.60 Hz, 4H, Ar), 7.50-6.80 (m, 44 H, Ar), 3.46 (br, 4H, CH2); 31P{1H} NMR: 253 K 18.1 (br), -30.4 (br) ppm; 298 K 16.8 (vbr), -28.1 (vbr) ppm; 333 K -23.3 (vbr) ppm; IR(KBr) 3053w, 2932w, 1431s, 1313vs, 1159vs, 994s, 800s, 694s, 378m cm-1; Elemental Anal. Calc. for PtN2S4P4O4C64H52¡¤0.5CH2Cl2. Found: C, 55.42 (55.00); H, 3.79 (3.66); N: 2.00 (1.97)%.

27148-03-4, In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles.,27148-03-4 ,Benzo[d]isothiazole-3(2H)-thione 1,1-dioxide, other downstream synthetic routes, hurry up and to see

Reference£º
Article; Al-Jibori, Subhi A.; Al-Jibori, Mohamed H.S.; Hogarth, Graeme; Inorganica Chimica Acta; vol. 398; (2013); p. 117 – 123;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

As a common heterocyclic compound, it belongs to isothiazole compound, name is 3-Bromoisothiazole, and cas is 55512-82-8, its synthesis route is as follows.

To a reaction flask were added compound 5 (200 mg, 0.392 mmol), 3-bromoisothiazole (96 mg, 0.588 mmol), Pd(dppf)Cl2 (32 mg, 0.02 mmol) and sodium carbonate (126 mg, 1.18 mmol), 2 mL glycol dimethyl ether and 0.4 mL water were added, bubbled with nitrogen gas for 10 minutes, heated to 120 C in microwave and reacted for 0.5 hour. After TLC detected the reaction was complete, the reaction was concentrated, purified by silica gel column chromatography to afford 84 mg of a product, yield: 46%. LC-MS(APCI): m/z = 467.3(M+1)+; 1H NMR (400 MHz, DMSO) delta 10.17 (s, 1H), 9.04 (s, 1H), 8.90 (s, 1H),8.76 (d, J = 2.3 Hz, 1H), 8.05 (d, J = 2.3 Hz, 1H), 7.86 (d, J = 9.1 Hz, 2H), 7.33 (d, J = 8.8 Hz, 2H), 4.86 (d, J = 3.4 Hz, 1H), 4.21 (s, 1H), 3.41 (dd, J = 17.0, 9.3 Hz, 1H), 3.29 – 3.18 (m, 2H), 2.90 (d, J = 11.1 Hz, 1H), 1.89 – 1.80 (m, 1H), 1.75 (s, 1H).

55512-82-8, In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles.,55512-82-8 ,3-Bromoisothiazole, other downstream synthetic routes, hurry up and to see

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

As a common heterocyclic compound, it belongs to isothiazole compound, name is 3,4-Dichloroisothiazole-5-carboxylic acid, and cas is 18480-53-0, its synthesis route is as follows.

SYNTHESIS EXAMPLE 1 Process (a): After thionyl chloride (10 ml) had been added to 3,4-dichloro-5-isothiazole-carboxylic acid (0.99 g), the mixture was refluxed by heating for 2 hours. The excess of thionylchloride was then distilled off under reduced pressure, and 3,4-dichloro-5-isothiazolecarboxylic acid chloride was obtained.

18480-53-0, In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles.,18480-53-0 ,3,4-Dichloroisothiazole-5-carboxylic acid, other downstream synthetic routes, hurry up and to see

Reference£º
Patent; Assmann, Lutz; Kitagawa, Yoshinori; Ishikawa, Koichi; Yamazaki, Daiei; Sawada, Haruko; Araki, Yasuo; Sakuma, Haruhiko; Kinbara, Taro; Imanishi, Kinya; US2003/13750; (2003); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com