Tag: M.W:200-300

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.88982-82-5,4-Bromo-1,3-thiazole-2-carboxylic acid,as a common compound, the synthetic route is as follows.

To a suspension of 4-bromothiazole-2-carboxylic acid (CAS 88982-82-5) (0.1 12 g, 0.538 mmol) in DCM (5.38 mL) and DMF (8.34 mu, 0.108 mmol) was added oxalyl chloride (0.059 mL, 0.67 mmol) and this was stirred at room temperature. After 30 minutes the reaction was concentrated. The solid was dissolved in DCM (5.38 mL), and methyl 2-(2- aminophenyl)acetate hydrochloride (CAS 35613-44-6) (0.089 g, 0.538 mmol) and DIPEA (0.188 mL, 1 .077 mmol) were added and the reaction was stirred at room temperature. After 5 minutes the reaction was partially concentrated and then purified directly by flash chromatography (0-50% EtOAc: Heptanes) to provide the title compound. MS (ESI-) m/z 353.1 , 355.1 (M-H).

88982-82-5, 88982-82-5 4-Bromo-1,3-thiazole-2-carboxylic acid 15122065, athiazole compound, is more and more widely used in various fields.

Reference£º
Patent; NOVARTIS AG; BELANGER, David B.; FLOHR, Stefanie; GELIN, Christine Fang; JENDZA, Keith; JI, Nan; LIU, Donglei; LORTHIOIS, Edwige Liliane Jeanne; KARKI, Rajeshri Ganesh; MAINOLFI, Nello; POWERS, James J.; RANDL, Stefan Andreas; ROGEL, Olivier; VULPETTI, Anna; YOON, Taeyoung; WO2015/9977; (2015); A1;,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica

777-12-8, 6-(Trifluoromethyl)benzo[d]thiazol-2-amine is a thiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred solution of methyl 5-chloro-3-(2-(dimethylamino)ethyl)-2- methoxybenzoate (88mg, 0.324mmol) in methanol (5ml) was added IN potassium hydroxide (91mg, 1.62mmol, 1.62ml) solution. The mixture was heated at 60¡ãC overnight. IN HC1 was added to adjust the PH to 1. The mixture was concentrated in vacuo. The residue was dissolved in dimethylformamide (3ml). N,N,N’,N’-Tetramethyl-0-(lH-benzotriazol-l- yl)uronium hexafluorophosphate (71mg, 0.324mmol) was added followed by N,N- diisopropylethylamine (282ul, 1.62mmol). The resulting mixture was stirred at room temperature for 15mins, then 6-(trifluoromethyl)benzo[d]thiazol-2-amine (71mg, 0.324mmol) was added. The resulting mixture was stirred at 100¡ãC overnight. Saturated ammonium chloride solution was added and extracted with ethyl acetate for two times. The combined ethyl acetate layer was dried over Na2S04 and concentrated under reduced pressure. The residue was purified via silica gel column chromatography to give title compound as a yellow powder (34mg, 23percent). 1H NMR (300 MHz, Chloroform-i ) delta 8.16 (s, 1H), 8.05 (d, J = 2.7 Hz, 1H), 7.91 (d, J = 8.6 Hz, 1H), 7.71 (dd, J = 8.5, 2.0 Hz, 1H), 7.50 (d, J = 2.7 Hz, 1H), 3.97 (s, 3H), 2.99 – 2.93 (m, 2H), 2.75 – 2.66 (m, 2H), 2.43 (s, 6H). MS (ESI) [M+H]+requires m/z 458.08, found m/z 458.15., 777-12-8

The synthetic route of 777-12-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; JIN, Shengkan; AUGERI, David J.; CAO, Bin; TAO, Hanlin; (126 pag.)WO2017/201313; (2017); A1;,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.61296-22-8,2-Amino-5-bromothiazole monohydrobromide,as a common compound, the synthetic route is as follows.

NEt3 (63.4mL, 455MMOL) was added to a stirred suspension of 5- BROMOTHIAZOL-2-YLAMINE hydrobromide (102. 7g, 379MMOL) in CH2C12 (1. 5L). After LH, TFAA (64.2mL, 455MMOL) was added dropwise at 0 C over 15MIN. The mixture was allowed to warm to 20 C over lh, before being stirred for an additional 2h. H20 (600mL) was added and the resulting precipitate was collected. The aqueous layer of the filtrate was separated and extracted with CHC13 (3 x 300mL). The combined organic extracts were washed with brine, dried (NA2S04), filtered and concentrated. The collected precipitate and residual solid were combined and triturated with ETOAC-N-C6HO4 to give N- (5-BROMOTHIAZOL-2-YL)-2, 2,2-trifluoroacetamide : No.H (CDC13) : 7.45 (s, 1H), 13.05 (br, 1H). N-BULI (253mL of a 1.58M solution in hexanes, 403MMOL) was added dropwise over 50MIN to a stirred solution of the above amide (50. 0G, 183mmol) in anhydrous THF (1.3L) AT-78 C. After 1. 5H, a solution of N-FLUOROBENZENESULFONIMIDE (86. 0G, 275mmol) in anhydrous THF (250mL) was added dropwise over 30min. The mixture was stirred for 3h, before being warmed up TO-30 C. H20 (300mL) was added and the mixture was filtered through a Celite pad. The solid collected and Celite were washed with ET20 (400mL) and H20 (400mL). The organic layer of the filtrate was separated and extracted with water (2 x 400mL). The combined aqueous layers were washed with Et2O (400ML), before being acidified to pH 6.5 with 2M HC1 and extracted with EtOAc (2 x 400mL). The combined organic extracts were washed with H20 (2 x 400mL) and brine, before being dried (MgS04), filtered and concentrated. Column chromatography (EtOAc- N-C6H14, 1: 3 to 1: 2) GAVE N- (5-FLUOROTHIAZOL-2-YL)-2, 2, 2-TRIFLUOROACETAMIDE : & (CDC13) : 7.13 (d, 1H). AcCl (12.6mL, 175MMOL) was added dropwise to a stirred solution of this amide (15.7g, 73MMOL) in MEOH (300mL) at 0 C. The mixture was stirred at 20 C for 30min, heated under reflux for lh, and finally concentrated in vacuo. The residual solid was triturated with THF to give the title compound: I5H (D2O) : 7.00 (d, 1H)., 61296-22-8

The synthetic route of 61296-22-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; OSI PHARMACEUTICALS, INC.; WO2004/72066; (2004); A1;,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.13743-09-4,2-Methyl-5-phenylthiazole-4-carboxylic acid,as a common compound, the synthetic route is as follows.,13743-09-4

(S)-7-Methyl-2-(2-methylpyrrolidin-2-yl)-1 H-benzo[d]imidazole hydrochloride (27; 25.2 mg, 0.1 mmol) is dissolved in DCM (0.2 ml) and DIPEA (0.072 ml, 0.42 mmol) is added, followed by the addition of a solution of 2-methyl-5-phenylthiazole-4-carboxylic acid (28; 22 mg, 0.1 mmol), HATU (40 mg, 0.105 mmol) and DIPEA (80 mg, 0.62 mmol) in 0.5 ml DMF. Stirring is continued at RT for 16 h. The reaction mixture is diluted with DCM / MeOH = 1/1 (1 ml) followed by the addition of PL-HCCVresin (213 mg, 0.4 mmol) and stirring is continued for 2 h. The resin is filtered off, the solvent is evaporated under reduced pressure and the product is purified by preparative HPLC to give (S)-(2-methyl-2-(7-methyl-1 H- benzo[d]imidazol-2-yl)pyrrolidin-1 -yl)(2-methyl-5-phenylthiazol-4-yl)methanone (Ex. 5.1 ) as a colorless powder. LC-MS: tR = 1 .19 min; [M+H]+ = 417.31.

The synthetic route of 13743-09-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ACTELION PHARMACEUTICALS LTD; BOSS, Christoph; BROTSCHI, Christine; GUDE, Markus; HEIDMANN, Bibia; SIFFERLEN, Thierry; WILLIAMS, Jodi, T.; WO2013/182972; (2013); A1;,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.22900-83-0,Ethyl 2-bromo-4-methylthiazole-5-carboxylate,as a common compound, the synthetic route is as follows.

Tert-Butyl 4- (2-benzyl) -4 (trifluoromethyl) phenyl) piperazine-1-carboxylate(0. 52 g, 1.50 mmol),Bromo-4-methylthiocono-5-carboxylate (0.39 g, 1. 58 mmol) and potassium carbonate(0.42 g, 3. OO mmol) was addedDMSO (10 mL), and the reaction was allowed to warm to 110 ¡ã C for 20 hours.After completion of the reaction, the reaction solution was cooled to room temperature,And water (20 mL) was added thereto, followed by extraction with ethyl acetate (20 mLX3). The combined organic phases were dried over anhydrous sodium sulphateDried, filtered and the filtrate was concentrated under reduced pressure. The resulting residue was purified by silica gel column chromatography (petroleum ether / ethyl acetate (v / v) = 2/1)Afforded the title compound as a light yellow solid (0.35 g, 45.2percent)., 22900-83-0

The synthetic route of 22900-83-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Ru yuan yaozu zizhixian dazhong yaopin maoyi youxian co ltd/Ru yuan yaozu zizhixian dazhong yaopin maoyi youxian gongci; Jin, chuan Fei; Liang, Haiping; zhang, yingjun; Zhang, Ji; Kang, Ning; Li, Yong; Liu, Yan Ping; (38 pag.)CN105294554; (2016); A;,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica

944804-88-0, tert-Butyl 4-bromothiazol-2-ylcarbamate is a thiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

944804-88-0, A mixture of 48 (3.61g, 12.9mmol) and 70 Na2CO3 (3.4g, 32.3mmol) in DME/H2O/dioxane (240/48/48mL) was exchanged with N2 twice, and 5-chloro-2-fluoro-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine (45a) (6.6g, 25.9mmol) and Pd(PPh3)4 (1.45g, 1.25mmol) were added to the mixture. The reaction mixture was heated to 100C and stirred for 6h under N2 atmosphere. The solid was removed by centrifugation at 3000rpm, 25C for 20min. The supernatant was concentrated and the crude product was purified by silica gel flash chromatography (eluting with ethyl acetate in petroleum ether 2-5%) to give 11 as a white solid (1.57g, yield=37%). 1H NMR (400MHz, DMSO-d6) delta 11.79 (s, 1H), 8.44 (s, 1H), 8.11 (s, 1H), 7.61 (s, 1H), 1.50 (s, 9H); LC/MS (ESI, m/z) 274.05 [M+H]+.

The synthetic route of 944804-88-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Wang, Beilei; Wu, Jiaxin; Wu, Yun; Chen, Cheng; Zou, Fengming; Wang, Aoli; Wu, Hong; Hu, Zhenquan; Jiang, Zongru; Liu, Qingwang; Wang, Wei; Zhang, Yicong; Liu, Feiyang; Zhao, Ming; Hu, Jie; Huang, Tao; Ge, Juan; Wang, Li; Ren, Tao; Wang, Yuxin; Liu, Jing; Liu, Qingsong; European Journal of Medicinal Chemistry; vol. 158; (2018); p. 896 – 916;,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica

65872-41-5, 2-(2-Aminothiazol-4-yl)-2-(methoxyimino)acetic acid is a thiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 1: Preparation OF 2A : (7R)-7-[(Z)-2-(2-Amino-5-chlorothiazol-4-yl)-2- (METHOXVIMINO) ACETAMIDO]-3- [ (4- (AMINOMETHYI)-1-PYDDINIO) METHYL]-3- CEPHEM-4-CARBOXYLATE Bis-trifluoroacetic Acid Salt (see Fig. 2) A. Preparation of 2-AMINO-5-CHLORO-A- .-4-THIAZOLEACETIC Acid (6) To 500mL OF DMF WERE ADDED 50.0 g (250MUNOL) OF 2-AMINO-A-(METHOXYIMINO)-4- THIAZOLEACETIC acid and 35g (260 mmol) OF N-CHLOROSUCCINIMIDE. The mixture was stirred at room temperature OVERNIGHT, after which time mass spectral analysis showed no more starting material to be present. The light brown solution was used without further purification., 65872-41-5

65872-41-5 2-(2-Aminothiazol-4-yl)-2-(methoxyimino)acetic acid 5486924, athiazole compound, is more and more widely used in various fields.

Reference£º
Patent; THERAVANCE, INC.; WO2005/5436; (2005); A2;,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.50850-93-6,Ethyl 2-aminobenzo[d]thiazole-6-carboxylate,as a common compound, the synthetic route is as follows.

Commercially available ester 1 (1.0g, 4.5mmol) was dissolved in anhydrous THF and the RB flask was cooled to 0C. Then LiAlH4 was added slowly and the flask was stirred at 0C for additional 10min. The flask was then stirred at room temperature for 24h. The reaction was then cooled, quenched with methanol, NH4Cl Rochelle’s salt and diluted with ethyl acetate (10ml). The organic layer was separated and the aqueous layer was extracted with additional ethyl acetate (3¡Á10ml). The organic layers were combined, dried over Na2SO4 and concentrated under vacuo on a rotary evaporator to obtain a yellow solid. The crude product was purified via gradient silica gel column chromatography using a mixture of CH2Cl2 and methanol (100:1 to 5:1) to obtain the desired alcohol as yellow solid 2 (420mg, 52%). (0009) 1H NMR (500MHz, CDCl3): delta 7.57 (d, J=0.9Hz, 1H), 7.35-7.46 (m, 1H), 7.25 (dd, J=8.2, 1.8Hz, 1H), 6.45 (br s, 1H), 4.53 (s, 2H), 4.0 (br s, 1H). (0010) 13C NMR (125MHz, CDCl3): delta 167.6, 150.5, 134.9, 130.6, 125.1, 119.4, 117.7, 64.2,., 50850-93-6

The synthetic route of 50850-93-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Dutta, Aloke K.; Santra, Soumava; Harutyunyan; Das, Banibrata; Lisieski, Michael J.; Xu, Liping; Antonio, Tamara; Reith, Maarten E.A.; Perrine, Shane A.; European Journal of Pharmacology; vol. 862; (2019);,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.41731-83-3,Ethyl 2-bromothiazole-5-carboxylate,as a common compound, the synthetic route is as follows.

Step 1: 2-Bromo-1,3-thiazole-5-carboxamide Into a 2 L round-bottom flask was added ethyl 2-bromothiazole-5-carboxylate (50.0 g, 212 mmol), THF (500 mL) and MeOH (250 mL). To this was added concentrated ammonium hydroxide in water (590 mL) and the reaction mixture was stirred at room temperature for 4 h. The solvents were removed under reduced pressure and the crude mixture poured into a separatory funnel containing brine (1 L). The aqueous layer was extracted with EtOAc (4*500 mL) and the combined organic layers were washed with brine, dried over Na2SO4, filtered and concentrated under reduced pressure.

41731-83-3, The synthetic route of 41731-83-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Isabel, Elise; Lachance, Nicolas; Leclerc, Jean-Philippe; Leger, Serge; Oballa, Renata M.; Powell, David; Ramtohul, Yeeman K.; Roy, Patrick; Tranmer, Geoffrey K.; Aspiotis, Renee; Li, Lianhai; Martins, Evelyn; US2011/301143; (2011); A1;,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.88982-82-5,4-Bromo-1,3-thiazole-2-carboxylic acid,as a common compound, the synthetic route is as follows.

Step A:4-bromothiazole-2-carboxylic acid (1,1.0 g, 4.8 mmol)Dissolved in ethylene glycol dimethyl ether (12mL)And water (4mL),Add 4-fluorophenylboronic acid (17, 1.0 g, 7.2 mmol)And anhydrous potassium carbonate (994 mg, 7.2 mmol),Then tetrakis(triphenylphosphine)palladium (277 mg, 0.24 mmol) was added.The resulting mixture was heated to 98 C under nitrogen for 24 hours.TLC analysis indicated the end of the reaction.The reaction solution was cooled to room temperature.Then add water (40 mL),The pH was adjusted to 2-3 with 6M hydrochloric acid.Filtered, the filter cake was dissolved in 20 mL of dichloromethane.The dichloromethane layer was washed with a saturated sodium bicarbonate solution.Divide the water layer,Adjust the pH of the water layer to 2-3,Filter the suspension,The filter cake was dried to give compound 18 (906 mg).Yield: 84.7%.

88982-82-5, 88982-82-5 4-Bromo-1,3-thiazole-2-carboxylic acid 15122065, athiazole compound, is more and more widely used in various fields.

Reference£º
Patent; Zhejiang Haizheng Pharmaceutical Co., Ltd.; Wang Haibo; Zheng Xiaohe; Cai Zhengjiang; Zheng Shan; Ye Zhengchun; Ma Huidan; Lin Haiming; (54 pag.)CN108623532; (2018); A;,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica