Category: 2854-16-2

2854-16-2, With the rapid development and complex challenges of chemical substances, the synthesis of new drugs is usually one of the most effective ways to increase yield.2854-16-2, name is 1-Amino-2-methylpropan-2-ol, molecular formula is C4H11NO, molecular weight is 89.14, as common compound, the synthetic route is as follows.

j0086J To a 15 L glass reactor purged with nitrogen was charged Compound 14 (1.038 kg, 2.47 mol, 1 eq), followed by Me-THF (6.176 kg) and DIEA (0.384 kg, 2.97 mol, 1.2 eq). The resulting mixture was stirred at room temperature and then 1-amino-2-methylpropan-2-ol(0.265 kg, 2.97 mol, 1.2 eq) in Me-THF (2.647 kg) was slowly charged while maintaining 20-30 ¡ãC. After the reaction was complete, water (2.6 L) and n-heptane (2.076 kg) were added. The mixture was stirred for 20 mm., the aqueous layer was removed, water (2.6 L) was added and the pH of the aqueous phase adjusted to 7 using 0.1N HC1. The aqueous layer was removed, and the organic layer was washed with water (2 x 2.6 L), 4percent NaHCO3 (1.1 L), and water (1.15 L). The organic layer was concentrated under vacuum to 3.4 L. Me-THF (4.950 kg) was added, and the mixture was concentrated to 3.4 L. The residue was diluted with Me-THF (4.931 kg). The solution was clarified through a 1.2 t in-line filter. The clarified solution was concentrated to 2.6 L. The residue was heated to 45 ¡ãC, and then n-heptane (2.599 kg) was added slowly while maintaining 45 ¡ãC. The batch was seeded with 2-methyl-i -((4-(6-(trifluoromethyl)pyridin-2-yl)- 6-((2-(trifluoromethyl)pyridin-4-yl)amino)- 1,3,5 -triazin-2-yl)amino)propan-2-ol (lOg). nHeptane (2.599 kg) was added slowly while maintaining 45 ¡ãC. After ih, the batch was cooled down to 20 ¡ãC. The mixture was stirred at 20 C for ih. The batch was filtered. The solids were washed with n-heptane (2 x 1 L), and then vacuum-dried at 35 ¡ãC in an oven for 20 h. Isolated yield: 1.124 kg of 2-methyl-i -((4-(6-(trifluoromethyl)pyridin-2-yl)-6-((2- (trifluoromethyl)pyridin-4-yl)amino)- 1,3,5 -triazin-2-yl)amino)propan-2-ol (96 percent) as a light yellow powder.

Statistics shows that 2854-16-2 is playing an increasingly important role. we look forward to future research findings about 1-Amino-2-methylpropan-2-ol.

Reference:
Patent; AGIOS PHARMACEUTICALS, INC.; ZHANG, Shijie; (47 pag.)WO2017/24134; (2017); A1;,
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The major producers of chemicals have been the Europe, Japan and China. Due to the growing call for a cleaner, greener environment, people will have to find innovative ways to maintain their relevance. Here is a compound 2854-16-2, name is 1-Amino-2-methylpropan-2-ol. This compound has unique chemical properties. The synthetic route is as follows. 2854-16-2

5-(2 ,4-dichloro-5-(3-fluoropyridin-2-yl)benzamido)- 1 -phenyl- 1 H-pyrazole-3-carboxylicacid (Example 107, 78 g, 166 mmol) was sonicated in DMF (300 mL) with N,Ndiisopropylethylamine (58 mL, 332 mmol) to give a clear solution, which was cooled to 10CC. TPTU (74 g, 249 mmol) was added portionwise and the mixture stirred at 10C for20 minutes. A solution of 1-amino-2-methylpropan-2-ol (22.1 g, 249 mmol) in DMF (50 mL) was added dropwise at 1000 and the mixture then allowed to warm to room temperature and stirred for 16 hours. The reaction mixture was partitioned between EtOAc (600 mL) and water (600 mL). The aqueous layer was separated and extracted with additional EtOAc (3 x 200 mL). The combined organic layers were washed withsaturated aqueous ammonium chloride solution (300 mL), water (5 x 200 mL), dried (magnesium sulphate) and concentrated in vacuo to give an orange oil. The oil was treated with acetonitrile (300 mL) and the resulting solid collected by filtration, washed with acetonitrile and dried under vacuum to afford the title compound as a colourless solid (60 g, 66%).1H NMR (400MHz, DMSO-d6): O ppm 1.09 (s, 6H), 3.21-3.22 (d, 2H), 4.63 (5, 1H), 6.93(5, 1H), 7.45-7.49 (m, 1H), 7.50-7.55 (t, 2H), 7.58-7.65 (m, 3H), 7.69 (5, 1H), 7.80-7.85(t, 1H), 7.87-7.95 (m, 2H), 8.56-8.58 (d, 1H), 10.89 (5, 1H).MS m/z 540.45 [M-Hr

Statistics shows that 2854-16-2 is playing an increasingly important role. we look forward to future research findings about 1-Amino-2-methylpropan-2-ol.

Reference:
Patent; PFIZER INC.; BAGAL, Sharanjeet Kaur; CUI, Jingrong Jean; GREASLEY, Samantha Elizabeth; LUNNEY, Elizabeth Ann; MCALPINE, Indrawan James; NAGATA, Asako; NINKOVIC, Sacha; OMOTO, Kiyoyuki; SKERRATT, Sarah Elizabeth; STORER, Robert Ian; WARMUS, Joseph Scott; WO2015/170218; (2015); A1;,
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Researchers who often do experiments know that organic synthesis is a process of preparing more complex target molecules from simple raw materials through one or more chemical reactions. Generally, it requires fewer steps,and cheap raw materials. 2854-16-2, name is 1-Amino-2-methylpropan-2-ol. A new synthetic method of this compound is introduced below., 2854-16-2

(a)N-(2-hydroxy-2-methyl-propyl)-3-methoxy-4-nitro-benzamideA mixture of 3-methoxy-4-nitrobenzoic acid (1 g, 5.07 mmcl), HATU (2.31 g, 6.1mmcl), and 1-amino-2-methyl-propan-2-ol (1.13 g, 12.7 mmol) in dichloromethane (20 mL) was stirred on an ice-cold water bath, and DiPEA (2.2 mL, 12.7 mmol) was added. After 10 mm the mixture was allowed to warm to room temperature and stirred for I h. The mixture was diluted with ethyl acetate (100 mL) and subsequently washed with 5percent sodium bicarbonate solution (3x 75 mL) water and brine, dried over sodium sulfate and concentrated in vacuo to yield 1.47 gof crude N-(2-hydroxy-2-methyl-propyl)-3-methoxy-4-nitro-benzamide (quant.).

At the same time, in my other blogs, there are other synthetic methods of this type of compound,2854-16-2, 1-Amino-2-methylpropan-2-ol, and friends who are interested can also refer to it.

Reference:
Patent; NETHERLANDS TRANSLATIONAL RESEARCH CENTER B.V.; DE MAN, Adrianus Petrus Antonius; BUIJSMAN, Rogier Christian; STERRENBURG, Jan Gerard; UITDEHAAG, Joost Cornelis Marinus; DE WIT, Joeri Johannes Petrus; ZAMAN, Guido Jenny Rudolf; WO2015/155042; (2015); A1;,
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2854-16-2 , The common heterocyclic compound, 2854-16-2, name is 1-Amino-2-methylpropan-2-ol, molecular formula is C4H11NO, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc., below Introduce a new synthetic route.

A dichloromethane (0.5 mL) solution of 1-(3-(cyclopropylcarbamoyl)-8-((4-methoxybenzyl)(methyl)ammno)imidazo[ 1 ,2-bj pyridazin-6-yl)- 1 H-indole-3-carboxylicacid (15 mg, 0.029 mmol), 1-amino-2-methylpropan-2-ol (7.86 mg, 0.088 mmol), N,NDiisopropylethylammne (0.026 mL, 0.147 mmol), and HATU (16.76 mg, 0.044 mmol)was stirred at room temperature. After 15 minutes the reaction became a clear brown solution, and was complete. It was concentrated to an oil, then loaded onto a 4g ISCO column for purification by flash chromatography, eluting with 0-100percent ethyl acetate inhexanes. The reaction afforded N-cyclopropyl-6-(3-((2-hydroxy-2-methylpropyl)carbamoyl)- 1H-indol- 1 -yl)-8-((4-methoxybenzyl)(methyl)amino)imidazo[1,2-bjpyridazine-3-carboxamide (17 mg, 0.026 mmol, 90percent yield) as a white solid. LC retention time 0.92 mm [Al. MS (ES+) m/z: 582 (MH).

The synthetic route of 2854-16-2 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; BRISTOL-MYERS SQUIBB COMPANY; WEINSTEIN, David S.; DUNCIA, John V.; SPERGEL, Steven H.; (76 pag.)WO2018/93968; (2018); A1;,
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2854-16-2, Each compound has different characteristics, and only by selecting the characteristics of the compound suitable for a specific situation can the compound be applied on a large scale. 2854-16-2, name is 1-Amino-2-methylpropan-2-ol. This compound has unique chemical properties. The synthetic route is as follows.

To a solution of 2,3-difluorobenzaldehyde (10 g, 70.4 mmol) in methanol (100 mL) was added 1- amino-2-methylpropan-2-ol (6.27 g, 70.4 mmol) and NaOH (7.04 mL, 7.04 mmol). It was stirred under nitrogen atmosphere for 1 h, and then NaBH4 (1.065 g, 28.1 mmol) was added portion wise over 10 min. The reaction was stirred at ambient temperature for 24 h. The crude product was purified by silica gel chromatography. The fractions were concentrated to give the title compound (10 g, 44.0 mmol, 62.5 percent yield) as an off-white solid. LC-MS: m/z: 216.13(M+H)+, 1.915min (ret. time).

While traditionally a conservative industry, chemical producers will need to modernize their PR strategies to stay relevant.we look forward to future research findings about 2854-16-2, 1-Amino-2-methylpropan-2-ol.

Reference:
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; ASTEX THERAPEUTICS LIMITED; BOEHM, Jeffrey Charles; CALLAHAN, James Francis; HEIGHTMAN, Thomas Daniel; KERNS, Jeffrey K.; WOOLFORD, Alison Jo-Anne; YAN, Hongxing; (252 pag.)WO2018/104766; (2018); A1;,
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2854-16-2, Adding a certain compound to certain chemical reactions, such as: 2854-16-2, 1-Amino-2-methylpropan-2-ol, can increase the reaction rate and produce products with better performance than those obtained under traditional synthetic methods. Here is a downstream synthesis route of the compound, 2854-16-2, blongs to alcohols-buliding-blocks compound.

To a solution of 2-bromo-5-chlorobenzaldehyde (1 g, 4.56 mmol) in methanol (20 mL) wasadded 1-amino-2-methylpropan-2-ol (0.406 g, 4.56 mmol) and 1 N NaOH (0.5 mL, 0.500 mmol) under nitrogen atmosphere. NaBH4 (0.345 g, 9.11 mmol) was added portion wise over 10 mm at 0 00 and stirred at ambient temperature for 72 h. The reaction mixture was evaporated underreduced pressure before was purified with flash chromatographyy to afford 1 -((2-bromo-5-chlorobenzyl)amino)-2-methylpropan-2-ol (1 g, 3.39 mmol, 74.4 percent yield). LC-MS m/z 291 .9 (M+H), 1 .62 mm (ret. time).

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,2854-16-2, its application will become more common.

Reference:
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; ASTEX THERAPEUTICS LIMITED; KERNS, Jeffrey K.; YAN, Hongxing; CALLAHAN, James Francis; HEIGHTMAN, Thomas Daniel; BOEHM, Jeffrey Charles; WOOLFORD, Alison Jo-Anne; (250 pag.)WO2016/203401; (2016); A1;,
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2854-16-2, As we all know, there are many different methods for the synthesis of a compound, and people can choose the synthesis method that suits their own laboratory according to the actual situation. 2854-16-2, name is 1-Amino-2-methylpropan-2-ol, molecular formula is C4H11NO, The compound is widely used in many fields, so it is necessary to find a new synthetic route. The downstream synthesis method of this compound is introduced below.

To a suspension of 2,4,6,8-tetrachloro-pyrimido[5,4-djpyrimidine (1) (3.50 g,i3.Oi mmol) in THF (200 mL) at -78¡ãC, i-amino-2-methyl-propan-2-ol (i.i7 mL, i2.36 mmol) in THF (20 mL) was added via syringe pump (during about 30 mm) followed byDIPEA (2.93 mL, i6.9i mmol) in THF (20 mL). The reaction mixture was stirred at -78¡ãC for additional 30 mi and then allowed to reach the room temperature. Water (250 mL) was added and the resulting suspension was extracted with EtOAc (3 x iOO mL). The combined organic extracts were washed with water (iSO mL), then with brine (iSO mL) and dried over solid anhydrous MgSO4. After filtration, the solvent was removed and the residue waspurified by flash column chromatography using gradient elution from PE/EtOAc (iO:4) toPE/EtOAc (i : i) to give 2-methyl-i -(2,6,8-trichloro-pyrimido[5,4-djpyrimidin-4-ylamino)-propan-2-ol (29)(3.67 g, 92percent yield). 300 MHz ?H NMR (CDC13, ppm): 7.70-7.58 (iH, m)3.70 (2H, d, J=6.i Hz) i.80 (iH, s) i.36 (6H, s). ESI-MS (m/z): 322, 324, 326, 328 [M+Hf?.

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. 2854-16-2, 1-Amino-2-methylpropan-2-ol, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; GALLEON PHARMACEUTICALS, INC.; DAX, Scott L.; MENCEL, James Joseph; OZOLA, Vita; SUNA, Edgars; SHUBIN, Kirill; (294 pag.)WO2017/3822; (2017); A1;,
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