Day: October 14, 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.28620-12-4,6-Nitro-2-benzothiazolinone,as a common compound, the synthetic route is as follows.

Compound 47 (0.5?mmol) was dissolved in 1?mL dry DMF. Potassium carbonate (0.75?mmol) and 1-bromopentyl chloride (1.2?mmol) were added to the solution. The mixture was stirred at 80?C overnight. The solvent was evaporated under reduced pressure. The residue was dissolved in ethyl acetate (10?mL) and washed with water (2?*?10?mL). The organic layer was dried over MgSO4 and evaporated under reduced pressure. The product was purified by silica gel column chromatography (dichloromethane/petroleum ether 50:50, v/v). A yellow powder was obtained: yield 69%; mp 55?+-?1?C; 1H NMR (CDCl3) delta 8.37 (d, J?=?2.3?Hz, 1H), 8.25 (dd, J?=?2.3; 8.9?Hz, 1H), 7.14 (d, J?=?8.9?Hz, 1H), 4.01 (t, J?=?7.5?Hz, 2H), 1.75 (m, 2H), 1.40 (m, 4H), 0.90 (t, J?=?7.0?Hz, 3H); LC-MS (APCI+) m/z 267.1 (MH+).

28620-12-4, 28620-12-4 6-Nitro-2-benzothiazolinone 641571, athiazole compound, is more and more widely used in various fields.

Reference£º
Article; Leleu-Chavain, Natascha; Baudelet, Davy; Heloire, Valeria Moas; Rocha, Diana Escalante; Renault, Nicolas; Barczyk, Amelie; Djouina, Madjid; Body-Malapel, Mathilde; Carato, Pascal; Millet, Regis; European Journal of Medicinal Chemistry; vol. 165; (2019); p. 347 – 362;,
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.556-90-1,2-aminothiazol-4(5H)-one,as a common compound, the synthetic route is as follows.

556-90-1, General procedure: To a solution of the pseudothiohydantoin 6a (139 mg, 1.2 mmol), and sodium acetate (328 mg, 4.0 mmol) in acetic acid (5 ml) was added 5-phenyl-2-furaldehyde 5a (172 mg,1.0 mmol) at 25C. The solution was refluxed at 135C for 12 h. The precipitate was filtered and washed with water and diethyl ether. The filter cake was dried under high vacuum to afford 230 mg (85%) of compound 7a as an orange solid.

556-90-1 2-aminothiazol-4(5H)-one 11175, athiazole compound, is more and more widely used in various fields.

Reference£º
Article; Jung, Michael E.; Ku, Jin-Mo; Du, Liutao; Hu, Hailiang; Gatti, Richard A.; Bioorganic and Medicinal Chemistry Letters; vol. 21; 19; (2011); p. 5842 – 5848;,
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.133840-96-7,2-Chloro-6-(trifluoromethoxy)benzo[d]thiazole,as a common compound, the synthetic route is as follows.

In a 250-mL round-bottom flask, 2-chloro-6-trifluoromethoxy-1,3-benzothiazole (5.36 g, 21.14 mmol) and 4-bromo-2-fluoroaniline (4.82 g, 25.36 mmol) were combined in 100 mL n-butanol containing 1% 4.0 M HCl in dioxane, and heated at 90 C. overnight. The mixture was cooled to rt and the solvent was removed under reduced pressure. Ethyl acetate (50 mL) was added, and the mixture was ultrasonicated by suspending the flask in an ultrasonication bath for 30 minutes. The mixture was filtered, and the filtrate was concentrated under reduced pressure. Acetonitrile (50 mL) was added to the mixture, which was then ultrasonicated for 30 minutes and then filtered to provide the product as a white solid (5 g, 58%). LC-MS m/z 409.1 (MH+), ret. time 4.02 min.

133840-96-7, The synthetic route of 133840-96-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Bayer Pharmaceuticals Corporation; US2004/224997; (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.5198-88-9,2-Bromothiazole-4-carboxylic acid,as a common compound, the synthetic route is as follows.,5198-88-9

Compound 134 (0.96 g, 3.85 mmol) was dried in the tared reaction flask and weighed. This was dissolved in 30 mL dichloromethane, and 10 mL dimethylformamide was added along with a magnetic stir bar. 2-Bromothiazole-4-carboxylic acid (800.6 mg, 3.85 mmol) was weighed out and added. Diisopropylethylamine (1.0 mL, 5.7 mmol) was added followed by HATU (1.901 g, 5.00 mmol) and the reaction was stirred at room temperature overnight. This was concentrated directly onto silica and purified by column chromatography. Concentrating, then drying the pure fractions on high vacuum afforded 1.158 g of the title compound 136 (69% yield). 1H NMR (300 MHz, DMSO-d6) delta 12.14 (s, 1H), 8.57- 8.48 (m, 2H), 8.44 (s, 1H), 7.91 (ddd, J = 11.5, 8.4, 1.3 Hz, 1H), 7.52 (ddd, J = 8.4, 4.6, 3.8 Hz, 1H), 5.34 (d, J = 6.9 Hz, 1H), 4.52 (tt, J = 9.1, 7.3 Hz, 1H), 4.05 – 3.91 (m, 1H), 2.86- 2.72 (m, 2H), 2.39 (qd, J = 8.6, 2.8 Hz, 2H). m/z = 438/440 (M+H)+ (bromine isotopes).

As the paragraph descriping shows that 5198-88-9 is playing an increasingly important role.

Reference£º
Patent; RIGEL PHARMACEUTICALS, INC.; KELLEY, Ryan; LI, Hui; HECKRODT, Thilo; CHEN, Yan; MCMURTRIE, Darren; TSO, Kin; TAYLOR, Vanessa; SINGH, Rajinder; YEN, Rose; MAUNG, Jack; (256 pag.)WO2016/172560; (2016); 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.7238-62-2,Ethyl 2-chloro-4-methylthiazole-5-carboxylate,as a common compound, the synthetic route is as follows.

EXAMPLE 39 Preparation of Ethyl 2-(2′,4′-Dichlorophenoxy)-4-Methyl-5-Thiazolecarboxylate. A mixture of 6.24 g (0.03 mole) of ethyl 2-chloro-4-methyl-5-thiazolecarboxylate, 4.89 g (0.03 mole) of 2,4-dichlorophenol, 4.14 g (0.03 mole) of potassium carbonate and 40 ml. of acetone was held at reflux for 89 hours. Acetone was removed under reduced pressure. The residue was treated with 50 ml. of water and extracted with ether. The ether solution was washed successively with saturated sodium bicarbonate, 30 ml. of 10% sodium hydroxide and 50 ml. of water. The ether solution was dried (MgSO4) and concentrated. The residue was recrystallized from hexane to give 5.8 g (58%) of ethyl 2-(2′,4′-dichlorophenoxy)-4-methyl-5-thiazolecarboxylate as a white solid, m.p. 71-73 C. Anal. Calc’d. for C13 H11 Cl2 NO3 S: C, 47.00; H, 3.34; N, 4.22; Cl, 21.34. Found: C, 47.04; H, 3.34; N, 4.21; Cl, 21.36., 7238-62-2

As the paragraph descriping shows that 7238-62-2 is playing an increasingly important role.

Reference£º
Patent; Monsanto Company; US4199506; (1980); A;,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica

3364-80-5, Thiazole-4-carboxaldehyde is a thiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

3.3.C 3.3[0210] (S)-3-Phenyl-N-(3-(pyridin-4-yl)isoxazol-5-yl)-2-(thiazol-4- ylmethylamino)propanamide (3.3). To a 20 ml vial were added (S)-2-amino-3-phenyl-N- (3-(pyridin-4-yl)isoxazol-5-yl)propanamide 3.3.C (40 mg, 0.13 mmole), thiazole-4- carbaldehyde (18 mg, O.lbetammole), sodium triacetoxyborohydride (55 mg, 0.26mmole) and 10 ml of DCE. The reaction was stirred at 700C for 12 hours. The crude material was partitioned between DCM and water and then purified by reverse phase preparative HLPC to give (S)-3-phenyl-N-(3-(pyridin-4-yl)isoxazol-5-yl)-2-(thiazol-4- ylmethylamino)propanamide TFA salt 3.3 as a white solid (14.2 mg, 27 percent yield). LCMS ESI (pos.) m/e: 406.1 (M+l): IH NMR (500 MHz, MeOH-J) delta ppm 9.09 (d, J=I.96 Hz, 1 H), 8.87 (br. s., 2 H), 8.27 (d, J=5.38 Hz, 2 H), 7.77 (d, J=I.96 Hz, 1 H), 7.27 – 7.35 (m, 3 H), 7.20 – 7.25 (m, 2 H) 7.07 (s, 1 H), 4.42 – 4.55 (m, 2 H), 4.35 (dd, J=8.80, 5.87 Hz, 1 H), 3.44 (dd, J=13.57, 5.99 Hz, 1 H), 3.26 (dd, J=13.69, 8.80 Hz, 1 H).

3364-80-5, As the paragraph descriping shows that 3364-80-5 is playing an increasingly important role.

Reference£º
Patent; AMGEN INC.; DU, Xiaohui; FU, Zice; HOUZE, Jonathan, B.; JIAO, Xianyun; KIM, Yong-jae; LI, Leping; LIU, Jinqian; LIZARZABURU, Mike; MEDINA, Julio; SHEN, Wang; TURCOTTE, Simon; YU, Ming; WO2010/93849; (2010); 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.170235-26-4,Methyl 2-bromothiazole-4-carboxylate,as a common compound, the synthetic route is as follows.

Example 76; Preparation of Compound 76A and 76B; To a suspension of NaH (60% dispersion in oil, 10 mmol, 0.48 g.) in anhydrous dioxane (5 mL) was added a solution of indazole (10 mmol, 1.18 g) in dioxane (5 ml.) and the resulting reaction was allowed to stir for 30 minutes. A solution of 2- bromo-thiazole-4-carboxylic acid methyl ester (10.0 mmol, 2.22 g) in dioxane (5 mL) was then added dropwise and the reaction mixture was heated to 100C for 4 hrs. The reaction mixture was cooled to room temperature, quenched with water, and the solution was adjusted to pH 2 using 1 N HCI. The resulting basic solution was extracted with ethyl acetate and the organic phase was washed with water and brine, dried over anhydrous sodium sulfate, then filtered and concentrated. LCMS of the resulting residue showed two peaks for the acid indicating the formation of two regioisomers (Compounds 76A and 76B). HPLC-MS RT= 1.35 and 1.45 min, mass calculated for formula CnH7N3O2S 245.03, observed LCMS m/z 246.1 (M+H)., 170235-26-4

170235-26-4 Methyl 2-bromothiazole-4-carboxylate 2763213, athiazole compound, is more and more widely used in various fields.

Reference£º
Patent; SCHERING CORPORATION; WO2008/54749; (2008); A1;,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica

911052-85-2, (5-Bromothiazol-2-yl)methanol is a thiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

911052-85-2, (4-Bromo-thiazol-2-yl)-methanol (L. LG, 5.7 mmol) in DMF (15 ml) is treated at room temperature under nitrogen atmosphere with TRIFLUOROMETHANESULFONYL chloride (0.61 ml, 1 equivalent), and Et3N (0.8 ml, 1 equivalent). The reaction mixture is stirred for 3 hours at room temperature before the addition of sodium azide (1. 11 g, 3 equivalents), followed by overnight stirring at the same temperature. The reaction mixture is diluted with water and extracted with DCM and diethyl ether. The combined organic extracts are dried (MGSO4) and concentrated under reduced pressure to afford the crude product, which is used without purification in the next step.

The synthetic route of 911052-85-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ARRAY BIOPHARMA, INC.; WO2004/46101; (2004); 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.3364-78-1,2-(Chloromethyl)thiazole,as a common compound, the synthetic route is as follows.

To a solution of dimethylphosphine borane 1-25 (200 mg, 2.6 mmol) in THF (30 mL) at 0C was added NaH (60% dispersion in mineral oil, 1 12 mg, 2.8 mmol) in one portion whereupon effervescence was observed. The opaque reaction was stirred at rt for 10 min then cooled back to 0C whereupon 2-(chloromethyl)thiazole 1-45 (341 mg, 2.6 mmol) and Nal (383 mg, 2.6 mmol) were added. The mixture was allowed to warm to rt O/N, then water (10 mL) and DCM (10 mL) were added and the phases separated. The aqueous phase was extracted with DCM (2 x 15 mL) and the combined organic extracts washed with brine (20 mL) before passing through a phase separator cartridge (Biotage). Concentration in vacuo gave the crude product which was purified by column chromatography (Biotage Isolera 4, KP-Sil 25 g) eluting with DCM to 3% MeOH in DCM to provide the title compound as a yellow oil (73 mg, 0.4 mmol, 16%)., 3364-78-1

As the paragraph descriping shows that 3364-78-1 is playing an increasingly important role.

Reference£º
Patent; AUSPHERIX LIMITED; HOLMES, Ian; NAYLOR, Alan; ALBER, Dagmar; POWELL, Jonathan Raymond; MAJOR, Meriel Ruth; NEGOITA-GIRAS, Gabriel; ALLEN, Daniel Rees; GUETZOYAN, Lucie Juliette; KING, Nigel Paul; (199 pag.)WO2017/93543; (2017); 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.3622-23-9,2,6-Dichloro-1,3-benzothiazole,as a common compound, the synthetic route is as follows.

REFERENCE EXAMPLE 76 To a solution of 5-chloro-1,3-benzenediamine (1.5 g) in tetrahydrofuran (30 ml) was added slowly a 1.5M solution of n-butyl lithium in n-hexane (5.61 ml) at 0 C. The resultant mixture was stirred for 30 minutes at 0 C. To the mixture was added a solution of 2,6-dichlorobenzothiazole (429 mg) in tetrahydrofuran (5 ml). After stirring for 15 minutes at 0 C. and for an hour at ambient temperature, the reaction mixture was poured into a mixture of water and ethyl acetate. The separated organic layer was washed well with 0.1N-hydrochloric acid (total 400 ml). After evaporation under reduced pressure, the residue was crystallized from methanol to give 5-chloro-N-(6-chlorobenzothiazol-2-yl)-benzene-1,3-diamine (171 mg). APCI-Mass: 312.20, 310.27 (m/z, (M+H)+) NMR(DMSO-d6, delta): 5.50(2H, s), 6.28(1H, t, J=1.9 Hz), 6.81(1H, t, J=1.9 Hz), 7.07(1H, t, J=1.9 Hz), 7.33(1H, dd, J=2.2, 8.6 Hz), 7.56(1H, d, J=8.6 Hz), 7.94(1H, d, J=2.2 Hz), 10.41(1H, s).

3622-23-9, The synthetic route of 3622-23-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Yamada, Akira; Spears, Glen; Hayashida, Hisashi; Tomishima, Masaki; Ito, Kiyotaka; Imanishi, Masashi; US2003/176454; (2003); A1;,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica