Month: August 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.56354-98-4,6-Aminobenzo[d]thiazol-2(3H)-one,as a common compound, the synthetic route is as follows.

A mixture comprising 60.0 mg (307 mumol) 4-chloro-6-ethyl-5-methyl-7H-pyrrolo[2,3-d]pyrimidine (prepared according to intermediate exampLe 1a), 51 mg 6-amino-1,3-benzothiazol-2(3H)-one (CAS-No: 56354-98-4), 1.75 mL ethanol and 16.9 muL hydrochloric acid (4M in dioxane) was reacted at 110C for 10 hours. The residue was digested in a mixture of diethyl ether and ethanol and dried to give 85.3 mg (85%) of the title compound. 1HNMR (DMSO-d6): delta = 1.16 (3H), 2.37 (3H), 2.66 (2H), 7.23 (1H), 7.37 (1H), 7.74 (1H), 8.10 (1H), 9.65 (1H), 12.18 (1H), 12.50 (1H) ppm.

As the paragraph descriping shows that 56354-98-4 is playing an increasingly important role.

Reference£º
Patent; BAYER PHARMA AKTIENGESELLSCHAFT; KLAR, Ulrich; WORTMANN, Lars; KETTSCHAU, Georg; PUeHLER, Florian; LIENAU, Philip; PETERSEN, Kirstin; HAeGEBARTH, Andrea; SUeLZLE, Detlev; WO2014/44691; (2014); A1;,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica

88982-82-5, 4-Bromo-1,3-thiazole-2-carboxylic acid is a thiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 4-bromothiazole-2-carboxylic acid 11 (25.0 mg, 0.12 mmol) in DCM (2.0 mL), oxalyl chloride (0.02 mL,0.23 mmol) was added dropwise, and then DMF (2 drops) was added. The mixture was stirred at room temperature for 2 h and concentrated, dried by vacuum. DCM(3.0 mL) was added to the mixture and the mixture was cooled to 0 C and 3-aminobenzonitrile (60.0 mg, 0.51 mmol), DIEA (0.03 mL,0.17 mmol) was added. The mixture was stirred at room temperature overnight. The subsequent mixture was concentrated under reduced pressure and extractedwith H2O/ethyl acetate. The combined organic layer was dried by Na2SO4,concentrated under reduced pressure and purified by column chromatography on silica gel (hexane/ethyl acetate = 5:1) to afford the title compound 6be (16.0 mg, 43 %) as white solid: 1H-NMR (400MHz, CDCl3) delta 9.05(s, 1H), 8.16 (d, J = 1.64 Hz, 1H),7.86 (dt, J = 7.60, 1.92 Hz, 1H),7.59 (s, 1H), 7.48 (m, 2H). 13C-NMR (100 MHz, CDCl3) delta 163.2, 156.2, 137.6, 130.2, 128.5, 126.0,124.4, 123.9, 123.0, 118.2, 113.5. LC/MS (ESI-) 305.9 (M-H)+.

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

Reference£º
Article; Vu, Hoang Nam; Kim, Ji Young; Hassan, Ahmed H.E.; Choi, Kihang; Park, Jong-Hyun; Park, Ki Duk; Lee, Jae Kyun; Pae, Ae Nim; Choo, Hyunah; Min, Sun-Joon; Cho, Yong Seo; Bioorganic and Medicinal Chemistry Letters; vol. 26; 1; (2016); p. 140 – 144;,
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.

A mixture of compound IE (2.2 g, 10.0 mmol), N-methylpiperazine (1.1 g, 11.0 mmol), and K2C03 (3.4 g, 24.9 mmol) in acetonitrile (70 mL) was stirred at 80 C for 24 h. The mixture was concentrated and diluted with H20 and extracted with EtOAc (3x). The combined organic layers were dried and then concentrated to give compound 1G (2.5 g, >100%) as a brown solid. 1H NMR (400 MHz, CDC13) delta 7.85 (s, 1H), 4.28 (q, J = 1.2 Hz, 2H), 3.58 (t, J = 5.6 Hz, 4H), 2.50 (t, J = 5.6 Hz, 4H), 2.33 (s, 3H), 1.32 (t, J = 1.2 Hz, 3H).

41731-83-3 Ethyl 2-bromothiazole-5-carboxylate 3614103, athiazole compound, is more and more widely used in various.

Reference£º
Patent; NEUROPORE THERAPIES, INC.; STOCKING, Emily, M.; WRASIDLO, Wolfgang; WO2015/116663; (2015); A1;,
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Thiazole | chemical compound | Britannica

51640-36-9, 2-Chlorothiazole-5-carbonitrile is a thiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To an NMP (1 mL) solution of (fraiis)-/V-(azetidin-3-yl)-3-(5-fluoro-2- methoxyphenoxy)cyclobutanecarboxamide, trifluoroacetic acid salt (Intermediate 71 ) (27 mg, 0.066 mmol) and 2-chlorothiazole-5-carbonitrile (14 mg, 0.099 mmol) in a microwave reaction vial was added N,N-diisopropylethylamine (0.04 mL, 0.2 mmol). The reaction was heated in a microwave (145 C) for 1 .5 h, concentrated and loaded onto a semi-prep HPLC (TFA as modifier) for purification. The purified sample was dissolved in DCM, washed with saturated aqueous NaHCC>3 solution, and then concentrated to afford the title compound as a pale yellow solid (22 mg, 84%). 1H NMR (400 MHz, CDCI3) delta 2.53 (ddd, J = 13, 10, 6 Hz, 2 H), 2.75 (ddd, J = 14, 7, 4 Hz, 2 H), 2.96-3.09 (s, 1 H), 3.82 (s, 3 H), 4.04 (dd, J = 10, 5 Hz, 2 H), 4.50 (t, J = 9 Hz, 2 H), 4.92-5.01 (m, 2 H), 5.96 (d, J = 7 Hz, 1 H), 6.46 (dd, J = 10, 3 Hz, 1 H), 6.60 (td, J = 8, 3 Hz, 1 H), 6.79 (dd, J = 9, 5 Hz, 1 H), 7.68 (s, 1 H); LC-MS (LC-ES) M+H = 403.

As the paragraph descriping shows that 51640-36-9 is playing an increasingly important role.

Reference£º
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; DEATON, David Norman; GUO, Yu; HANCOCK, Ashley Paul; SCHULTE, Christie; SHEARER, Barry George; SMITH, Emilie Despagnet; STEWART, Eugene L.; THOMSON, Stephen Andrew; (556 pag.)WO2018/69863; (2018); A1;,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica

144164-11-4, Thiazol-5-ylmethyl ((2S,3S,5S)-5-amino-3-hydroxy-1,6-diphenylhexan-2-yl)carbamate is a thiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Thiazol-5-ylmethyl ((2S,3S,5S)-5-((S)-2-amino-3-methylbutanamido)-3-hydroxy-l ,6- diphenylhexan-2-yl)carbamate, compound C2: 526 mg (1.64 mmol, 1.0 eq) of TBTU was added to 356 mg (1.64 mmol, 1.0 eq) Boc-Val dissolved in 1.5 ml of DMF along with 690 mu of DIEA (3.94 mmol, 2.4 eq). The crude hydrolysate of RTV (700 mg, 1.64 mmol, 1.0 eq), dissolved in 1 ml of DMF, was added after 5 minutes of stirring in one portion. The reaction was left overnight and DMF was rotary evaporated. The reaction mixture was dissolved in 50 ml of EtOAc and washed two times by saturated NaHC03, two times with 10 % KHS04 and once with brine. The organic mixture was dried, evaporated and the product was purified using Flash chromatography (TLC analysis: EtOAc, R/ = 0.65). Product was further dissolved in 5 ml of hot EtOAc and 5 ml of diethyl ether was added. The resulting gel was filtrated and dried to give very pure (>99 %, HPLC) 250 mg of product (yield = 25 %). The product was then treated with TFA (approx. 1 ml) for 15 minutes, alternately sonicated and stirred. The remaining TFA was then removed by flow of nitrogen. The oily product was dissolved in water/ ACN and was lyophilisated. Analytical HPLC Rr = 17.4 min. HRMS (ESI+): calculated for C28H37O4N4S [M]+ 525.25300. Found 525.25292. NMR (500 MHz, DMSO-d6): 9.06 (d, 1H, 4/ = 0.8, N-CH-S), 8.24 (d, 1H / = 8.2, -NH-CO), 8.00 (bd, 3H, / = 5.2, -NH3+), 7.85 (q, 1H, 4J = 0.8, S-C-CH-N), 7.28-7.13 (m, 10H, Ph-), 6.94 (d, / = 9.4, 1H, NH-CO-O), 5.12 (d, 2H, 4J = 0.8, 0-CH2), 4.16 (m, 1H, CH-NH- CO), 3.78 (m, 1H, CH-NH3+, partial overlap with water residual peak), 3.58 (td, 1H, / = 6.8, / = 2.0, CH-OH), 3.48 (m, 1H, Ph-CH2-CH-NH), 2.72-2.67 (m, 4H, 2xCH-CH2-Ph), 2.00 (m, 1H, CH-(CH3)2), 1.50 (m, 1H, OH-CH-CH2), 1.43 (m, 1H, OH-CH-CH2), 0.89 (d, 3H, / = 6.8 -CH3), 0.84 (d, 3H, / = 6.8 -CH3). 13C NMR (125.7 MHz, DMSO-d6): 167.33 (CO Val), 158.33(q, /CF = 34.4, CF3COO-), 155.79 (O-C-N), 155.71 (N-CH-S), 143.23 (S-C-CH-N), 139.50 (Ph), 138.55 (Ph), 134.23 (S-C-CH-N), 129.56 (Ph), 129.17 (Ph), 128.30 (Ph), 128.25 (Ph), 126.26 (Ph), 126.09 (Ph), 116.44 (q, JQF = 294.8, CF3-COO ) 68.90 (HO-CH), 57.56 (CO-CH-NH3), 57.44 (COO-CH2), 55.74 (HO-CH-CH-NH), 47.98 (CONH-CH), 39.75 (NH-CH-CH2-Ph), 37.77 (-CH2-CH-CH-), 37.33 (Ph-CH2-CH-NH), 30.04 (CH(CH3)2), 17.26 and 18.69 (2xCH3).

144164-11-4 Thiazol-5-ylmethyl ((2S,3S,5S)-5-amino-3-hydroxy-1,6-diphenylhexan-2-yl)carbamate 11101978, athiazole compound, is more and more widely used in various.

Reference£º
Patent; USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I.; USTAV MAKROMOLEKULARNI CHEMIE AV CR, V.V.I.; UNIVERZITA KARLOVA V PRAZE, PRIRODOVEDECKA FAKULTA; SACHA, Pavel; KONVALINKA, Jan; SCHIMER, Jiri; KNEDLIK, Tomas; NAVRATIL, Vaclav; TYKVART, Jan; SEDLAK, Frantisek; MAJER, Pavel; CIGLER, Petr; SUBR, Vladimir; ULBRICH, Karel; STROHALM, Jiri; (53 pag.)WO2016/112883; (2016); A2;,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica

4175-76-2, 2,4-Dichlorothiazole is a thiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Preparation 194-chloro-2-morpholino-thiazoleTo a mixture of 2,4-dichlorothiazole (34 g, 0.22 mol) in acetonitrile (425 mL) add potassium carbonate (60.9 g, 0.44 mol) and then morpholine (21.2 mL, 0.225 mol) dropwise over 30 min. Reflux the mixture at 40 0C and then cool to 22 C. Filter the mixture and evaporate the filtrate. Triturate the residue with /-propyl alcohol (60 mL) at 22 0C for one hour. Filter the solids and dry under vacuum to a constant weight to afford the title compound (34.5 g, 76%). ES/MS m/z (35Cl) 205 (M+l)+.

As the paragraph descriping shows that 4175-76-2 is playing an increasingly important role.

Reference£º
Patent; ELI LILLY AND COMPANY; WO2008/36579; (2008); A1;,
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Thiazole | chemical compound | Britannica

934-34-9, Benzothiazolone is a thiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

6-(4-Nitrobenzoyl)-1,3-benzothiazol-2(3H)-one (1; Table I-B). In a 100 ml flask containing 35.0 g (265 mmol) aluminium chloride, add drop by drop and with magnetic stirring 5.9 ml of dimethylformamide (76 mmol). Continue stirring for 25 minutes, slowly add 5.0 g (33 mmol) of 2(3H)-benzothiazolone and heat to 90 C. Add drop by drop 7.36 g of 4-nitrobenzoyl chloride (40 mmol) and continue to stir at 100-110 C. for 4 hours. Slowly pour the reaction mixture onto ice while stirring vigorously. Add 15 ml of 37% hydrochloric acid and then stir for 15 minutes. Spin out the precipitate then wash with water until the wash water is neutral. Dry the product obtained and recrystallise it in dioxane (5.85 g, 59%). Rf=0.39 (EtOAc/Cyclohexane=4/6): mp 260-265 C.; ir gamma NH 3369 cm-1, CO 1682 cm-1, 1651 cm-1, NO2 1521 cm-1; 1H-NMR (300 MHz, DMSO-d6) delta 7.26 (d, 1H, H4, J4-5=7.8 Hz), 7.72-7.74 (m, 1H, H5), 7.92 (d, 2H, H3′, H5′, J=9.0 Hz), 8.09 (s, 1H, H7), 8.36 (d, 2H, H2′, H6′, J=9.0 Hz), 12.3 (br s, 1H, NH, exchangeable with D2O). Anal. (C14H8N2O4S)

The synthetic route of 934-34-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Park, Chang-Ha; Yous, Said; Nativelle-Serpentini, Celine; Seralini, Gilles-Eric; Chang, Soon-Jae; Lesieur, Daniel; US2007/54899; (2007); A1;,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica

29182-42-1, Ethyl 2-(benzo[d]thiazol-2-yl)acetate is a thiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

1-4. Synthesis of 3-(Benzo[d]thiazol-2-yl)-7-(isopropyl(prop-2-ynyl)amino)-2H-chromen-2-one Compound of Chemical Formula 1 To a solution in which the 2-hydroxy-4-(isopropyl(prop-2-ynyl)amino)benzaldehyde (1.8 g, 8.28 mmol) compound of Chemical Formula 4 was dissolved in ethanol (15 mL), ethyl 2-(benzo[d]thiazol-2-yl)acetate (1.83 g, 8.28 mmol) and piperidine (1.63 mL, 16.56 mmol) were added consecutively at room temperature. The reaction mixture was heated under reflux for 2 hours, cooled to room temperature, and 3-(benzo[d]thiazol-2-yl)-7-(isopropyl(prop-2-ynyl)amino)-2H-chromen-2-one (1.54 g, 50%) was obtained by filtering the precipitated solid. 1H NMR (500 MHz, CDCl3) d 8.94 (s, 1H), 8.02 (d, 1H, J=8.2 Hz), 7.94 (d, 1H, J=7.8 Hz), 7.54 (d, 1H, J=8.7 Hz), 7.47-7.50 (m, 1H), 7.35-7.38 (m, 1H), 6.88 (dd, 1H, J=2.3, 8.7 Hz), 6.80 (d, 1H, J=2.3 Hz), 4.21-4.26 (m, 1H), 4.04 (d, 2H, J=2.3 Hz), 2.26 (t, 1H, J=2.2 Hz), 1.34 (d, 6H, J=6.4 Hz); 13C NMR (125 MHz, CDCl3) d 161.5, 161.0, 156.7, 152.6, 152.4, 142.0, 136.4, 130.6, 126.2, 124.7, 122.3, 121.7, 113.9, 111.0, 109.8, 98.8, 80.0, 72.3, 49.5, 33.5, 20.2 (2).

As the paragraph descriping shows that 29182-42-1 is playing an increasingly important role.

Reference£º
Patent; ACCOBIOTECH SDN BHD.; GENBODY INC.; Park, Hyun; Kim, Hak Sung; Song, Hyun Ok; Chong, Chom Kyu; Kim, Sung Yeon; US2014/350227; (2014); A1;,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica

18903-18-9, Ethyl 5-aminothiazole-4-carboxylate is a thiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Intermediate 61 Sodium hydride (60% disp. in oil; 2.79g, 69.68mmol) was suspended in dry tetrahydrofuran (60m L). To this, 5-amino-thiazole-4-carboxylic acid ethyl ester (4g, 23.23mmol) was added at 0C and the mixture was stirred for 10 minutes. To this, 4- nitrobenzenesulfonyl chloride (6.2g, 27.87mmol) was added at 0C and the mixture stirred at room temperature for 2 hours. The mixture was diluted with ammonium chloride solution and diethyl ether. The solid formed collected by filtration, washed with ether and dried under vacuum to give Intermediate 61 (3.2g) as a yellow solid. LCMS (Method 37) Rt 1.56 min; m/z(M-H)” 356

18903-18-9 Ethyl 5-aminothiazole-4-carboxylate 12620181, athiazole compound, is more and more widely used in various.

Reference£º
Patent; ANTABIO SAS; LEMONNIER, Marc; DAVIES, David; PALLIN, David; WO2014/198849; (2014); 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.74370-93-7,4-(tert-Butyl)thiazol-2-amine,as a common compound, the synthetic route is as follows.

Synthesis of 2-bromo-4-tert-butylthiazole 85% strength phosphoric acid (50 ml) and 65% strength nitric acid (20 ml) were combined at 0 C. 3.12 g (20.0 mmol) of 4-tert-butylthiazol-2-ylamine were added to this solution and a solution of 1.38 g (20 mmol) of NaNO2 in water (10 ml) was subsequently added dropwise at 0 C. in the course of 30 min. The reaction solution was stirred at 0 C. 1 h and then added dropwise to a suspension of 20.0 g of NaBr and 5.8 g of CuBr in water (20 ml) cooled to 0 C. The mixture was stirred until evolution of gas could no longer be observed. Subsequently, the mixture was adjusted to a pH>10 using 50% strength aq. KOH solution and the product was separated off by steam distillation. The distillate was extracted with EE. The organic phase was dried over MgSO4, filtered, and concentrated in vacuo. 3.03 g (13.8 mmol, 69%) of 2-bromo-4-tert-butylthiazole were obtained as a residue.

The synthetic route of 74370-93-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Gruenenthal GmbH; US2007/112011; (2007); A1;,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica