Category: 1030377-21-9

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1030377-21-9,(S)-1-Boc-2-(Hydroxymethyl)piperazine,as a common compound, the synthetic route is as follows.

To a solution of (S)-l-Boc-2-hydroxymethylpiperazine (1.0 g, 4.62 mmol) in DCE (92.47 ml, 4.624 mmol) was added formaldehyde (3.474 ml, 46.24 mmol) (37% in water) followed by sodium triacetoxyborohydnde (4.9 g, 23.12 mmol). The mixture was stirred vigorously at room temperature for 2.5hours. The mixture was treated with saturated sodium bicarbonate (30 mL), stirred for 10 min then extracted with DCM (3 x 10 mL). The combined organic phases were dried over sodium sulfate, filtered and concentrated. ES+APCI MS m/z 231.1 [M+H]+., 1030377-21-9

The synthetic route of 1030377-21-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; MIRATI THERAPEUTICS, INC.; ARRAY BIOPHARMA, INC.; FISCHER, John, P.; FELL, Jay, Bradford; BLAKE, James, F.; HINKLIN, Ronald, Jay; MEJIA, Macedonio, J.; HICKEN, Erik, James; CHICARELLI, Mark, Joseph; GAUDINO, John, J.; VIGERS, Guy, P.A.; BURGESS, Laurence, E.; MARX, Matthew, Arnold; CHRISTENSEN, James, Gail; LEE, Matthew, Randolf; SAVECHENKOV, Pavel; ZECCA, Henry, J.; (529 pag.)WO2017/201161; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1030377-21-9,(S)-1-Boc-2-(Hydroxymethyl)piperazine,as a common compound, the synthetic route is as follows.

To a solution of (S)-l-Boc-2-hydroxymethylpiperazine (1.0 g, 4.62 mmol) in DCE (92.47 ml, 4.624 mmol) was added formaldehyde (3.474 ml, 46.24 mmol) (37% in water) followed by sodium triacetoxyborohydnde (4.9 g, 23.12 mmol). The mixture was stirred vigorously at room temperature for 2.5hours. The mixture was treated with saturated sodium bicarbonate (30 mL), stirred for 10 min then extracted with DCM (3 x 10 mL). The combined organic phases were dried over sodium sulfate, filtered and concentrated. ES+APCI MS m/z 231.1 [M+H]+., 1030377-21-9

The synthetic route of 1030377-21-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; MIRATI THERAPEUTICS, INC.; ARRAY BIOPHARMA, INC.; FISCHER, John, P.; FELL, Jay, Bradford; BLAKE, James, F.; HINKLIN, Ronald, Jay; MEJIA, Macedonio, J.; HICKEN, Erik, James; CHICARELLI, Mark, Joseph; GAUDINO, John, J.; VIGERS, Guy, P.A.; BURGESS, Laurence, E.; MARX, Matthew, Arnold; CHRISTENSEN, James, Gail; LEE, Matthew, Randolf; SAVECHENKOV, Pavel; ZECCA, Henry, J.; (529 pag.)WO2017/201161; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1030377-21-9, (S)-1-Boc-2-(Hydroxymethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,1030377-21-9

A suspension of 1-fluoro-4-nitrobenzene (1.305 g, 9.25 mmol), (S)-tert-butyl 2-(hydroxymethyl)piperazine-1-carboxylate (2.00 g, 9.25 mmol) and potassium carbonate (1.917 g, 13.87 mmol) in anhydrous DMF (10 mL) was heated to 50 C under a nitrogen atmosphere overnight. The reaction mixture was allowed to cool to room temperature, diluted with water (70 mL) and stirred at roomtemperature for 15 minutes. The precipitated solid was isolated by filtration, washed with water (50 mL), sucked dry and freeze-dried overnight to give the title compound as an orange solid (2.13 g, 68%) . ?H NMR (300 MHz, CDC13) 3 8.11 (dt, 2H), 6.78 (dt, 2H), 4.25 (br s, 1H), 3.85-4.04 (m, 2H), 3.61-3.80 (m, 3H), 3.25-3.43 (m, 2H), 3.18(ddd, 1H), 1.49 (s, 9H). LCMS (Method C): RT = 1.39 mm, m/z = 338 [M+H].

As the paragraph descriping shows that 1030377-21-9 is playing an increasingly important role.

Reference：
Patent; ALMAC DISCOVERY LIMITED; HARRISON, Timothy; TREVITT, Graham; HEWITT, Peter Robin; O’DOWD, Colin Roderick; BURKAMP, Frank; WILKINSON, Andrew John; SHEPHERD, Steven D.; MIEL, Hugues; WO2015/92431; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1030377-21-9,(S)-1-Boc-2-(Hydroxymethyl)piperazine,as a common compound, the synthetic route is as follows.

To a solution of(s)-i -boc-2-(hydroxymethyl)piperazine (5.0 g, 23.12 mmol) in i,2-dichloroethane (100 mL) was added benzaldehyde (7.04 mL, 69.4mmol). The resulting mixture was then stirred at room temperature for 30 mm, and then sodium triacetoxyborohydride (6.85 mL, 46.2 mmol) was added. The resulting mixture was then stirred at room temperature overnight. Then, the mixture was quenched with saturated NaHCO3 (20 mL) and was stirred at room temperature for 10 mm. The organic layer was collected and aqueous layer wasextracted with EtOAc (1 x 30 mL). The combined organic extracts were then dried over Mg504 and concentrated in vacuo. Chromatographic purification of the residue (silica gel, 0% to 100% EtOAc/heptane) provided (5)-tert-butyl 4- benzyl-2-(hydroxymethyl)piperazine- 1 -carboxylate (5.86 g, 19. 13 mmol, 83% yield) as an oil. MS (ESI, +ve ion) m/z 307.3 (M+H)., 1030377-21-9

The synthetic route of 1030377-21-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; AMGEN INC.; HARRINGTON, Paul E.; ASHTON, Kate; BROWN, Sean P.; KALLER, Matthew R.; KOHN, Todd J.; LANMAN, Brian Alan; LI, Kexue; LI, Yunxiao; LOW, Jonathan D.; MINATTI, Ana Elena; PICKRELL, Alexander J.; STEC, Markian M.; TAYGERLY, Joshua; (991 pag.)WO2018/183418; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1030377-21-9, (S)-1-Boc-2-(Hydroxymethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of (S)-tert-butyl 2-(hydroxymethyl)piperazine-l -carboxylate (850.9 mg, 3.93 mmol) and 2-(tert-butoxymethyl)oxirane (850 mg, 6.46 mmol) in ethanol (10 mL) was heated at 120 C for 30 min using microwave. The mixture was concentrated to dryness. The residue was purified with flash column chromatography on silica gel using 1-10% methanol in dichloromethane to afford a oil as the product in quantitative yield. 1H NMR (500 MHz, Chloroform-^ delta 4.09 (s, lH), 3.84 (m, 3H), 3.38 (dt, J= 9.0, 3.7 Hz, l H), 3.28 (m, 3H), 3.04 (dd, J = 24.2, 1 1.7 Hz, 1H), 2.88 – 2.80 (m, 2H), 2.48 – 2.32 (m, 3H), 2.26 – 2.21 (m, 1H), 2.13-2.08 (m, 1H), 1.44 (s, 9H), 1.17 (d, 9H). MS for ^Eta34Nu205: 347.2 (MH+).

1030377-21-9, 1030377-21-9 (S)-1-Boc-2-(Hydroxymethyl)piperazine 22884145, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; NEKTAR THERAPEUTICS (INDIA) PVT. LTD.; NEKTAR THERAPEUTICS; SHARMA, PANKAJ; KHATRI, VIJAY KUMAR; GU, XUYUAN; SONG, YUAN; SHEN, MICHAEL LIXIN; SAUTHIER, JENNIFER RIGGS; ANAND, NEEL K.; KOZLOWSKI, ANTONI; ODINECS, ALEKSANDRS; RILEY, TIMOTHY A.; REN, ZHONGXU; MU. YONGQI; SHEN, XIAOMING; YUAN. XUEJUN; AURRECOECHEA, NATALIA; O’MAHONY, DONOGH JOHN ROGER; WO2015/92819; (2015); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1030377-21-9, (S)-1-Boc-2-(Hydroxymethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 2: (S)-tert-butyl 4-(5-(1-(2-cyanophenyl)piperidin-4-ylamino)-2,4-dimethylbenzoyl)-2-(hydroxymethyl)piperazine-1-carboxylate The procedure for (S)-tert-butyl 4-(5-(1-(2-cyanophenyl)piperidin-4-ylamino)-2,4-dimethylbenzoyl)-2-(hydroxymethyl)piperazine-1-carboxylate was HATU generic method A. ESI-MS (EI+, m/z): 548.0 [M+H]+. 1H NMR (500 MHz, CD3OD-d4) delta: 7.55-7.62 (m, 2H), 7.20 (d, J=8.5 Hz, 1H), 7.06-7.09 (t, J=7.5 Hz, 1H), 6.96 (s, 1H), 6.49-6.58 (m, 2H), 3.47-4.32 (m, 9H), 2.97-3.21 (m, 5H), 2.10-2.22 (m, 8H), 1.77 (d, J=10.0 Hz, 2H), 1.48 (s, 9H)., 1030377-21-9

As the paragraph descriping shows that 1030377-21-9 is playing an increasingly important role.

Reference£º
Patent; Navitor Pharmaceuticals, Inc.; O’Neill, David John; Saiah, Eddine; Kang, Seong Woo Anthony; Brearley, Andrew; Bentley, Jonathan; (519 pag.)US2018/127370; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1030377-21-9, (S)-1-Boc-2-(Hydroxymethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,1030377-21-9

To (S)-2-hydroxymethyl-piperazine-1 -carboxylic acid fe/t-butyl ester (2.00 g, 9.25 mmol) in DMA (10 mL) is added ie f-butyl-chloro-dimethyl-silane (2.09 g, 13.9 mmol) and imidazole (1 .89 g, 27.7 mmol), and the reaction mixture is stirred for 24 h at rt. The reaction mixture is diluted with NH4CI-solution and extracted with EtOAc. The organic layer is washed with water and brine, dried over Na2S04, filtered and concentrated under reduced pressure. The residue is purified by silica gel column chromatography to give the title compound. (0573) Yield: 2.80 g (92%)

1030377-21-9 (S)-1-Boc-2-(Hydroxymethyl)piperazine 22884145, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; HYDRA BIOSCIENCES, INC.; BOUYSSOU, Thierry; GOTTSCHLING, Dirk; HEINE, Niklas; SMITH KEENAN, Lana Louise; LOWE, Michael D.; RAZAVI, Hossein; SARKO, Christopher Ronald; SURPRENANT, Simon; TAKAHASHI, Hidenori; TURNER, Michael Robert; WU, Xinyuan; (182 pag.)WO2019/81637; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1030377-21-9,(S)-1-Boc-2-(Hydroxymethyl)piperazine,as a common compound, the synthetic route is as follows.

A mixture of (S)-tert-butyl 2-(hydroxymethyl)piperazine-l -carboxylate (602.7 mg, 2.79 mmol) and (S)-2-methoxyoxirane (308.9 mg, 3.4 mmol) in ethanol (10 mL) was heated at 120 C for 30 min using microwave. The mixture was concentrated to dryness. The residue was purified with flash column chromatography on silica gel using 1 -10% methanol in dichloromethane to afford a oil as the product (794.6 mg) in 94% yield. NMR (500 MHz, Chloroform-*/) delta 4.11 (br, 1H), 3.93 – 3.80 (m, 2H), 3.41 (dd, J = 9.7, 3.7 Hz, 1H), 3.36 (s, 3H), 3.33 (dd, J = 9.7, 6.0 Hz, lH), 3.25 (br, 2H), 3.06 (d, J = 1 1.6 Hz, 1H), 2.89 (br, 2H), 2.79 (d, J = 1 1.2 Hz, 1H), 2.47 (dd, J = 12.7, 9.1 Hz, 1H), 2.49 – 2.33 (m, 1 H), 2.30 – 2.21 (m, 2H), 1.43 (s, 9H). MS for C,4H28N205: 305.2 (MH+).

1030377-21-9, As the paragraph descriping shows that 1030377-21-9 is playing an increasingly important role.

Reference£º
Patent; NEKTAR THERAPEUTICS (INDIA) PVT. LTD.; NEKTAR THERAPEUTICS; SHARMA, PANKAJ; KHATRI, VIJAY KUMAR; GU, XUYUAN; SONG, YUAN; SHEN, MICHAEL LIXIN; SAUTHIER, JENNIFER RIGGS; ANAND, NEEL K.; KOZLOWSKI, ANTONI; ODINECS, ALEKSANDRS; RILEY, TIMOTHY A.; REN, ZHONGXU; MU. YONGQI; SHEN, XIAOMING; YUAN. XUEJUN; AURRECOECHEA, NATALIA; O’MAHONY, DONOGH JOHN ROGER; WO2015/92819; (2015); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1030377-21-9,(S)-1-Boc-2-(Hydroxymethyl)piperazine,as a common compound, the synthetic route is as follows.

To a solution of (S)-l-Boc-2-hydroxymethylpiperazine (1.0 g, 4.62 mmol) in DCE (92.47 ml, 4.624 mmol) was added formaldehyde (3.474 ml, 46.24 mmol) (37% in water) followed by sodium triacetoxyborohydride (4.9 g, 23.12 mmol). The mixture was stirred vigorously at room temperature for 2.5hours. The mixture was treated with saturated sodium bicarbonate (30 mL), stirred for 10 min then extracted with DCM (3 x 10 mL). The combined organic phases were dried over sodium sulfate, filtered and concentrated. ES+APC1 MS m/z 231.1 [M+H]+., 1030377-21-9

As the paragraph descriping shows that 1030377-21-9 is playing an increasingly important role.

Reference£º
Patent; MIRATI THERAPEUTICS, INC.; ARRAY BIOPHARMA, INC.; MARX, Matthew, Arnold; BLAKE, James, F.; FELL, Jay, Bradford; FISCHER, John, P.; MEJIA, Macedonio, J.; (164 pag.)WO2020/47192; (2020); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1030377-21-9, (S)-1-Boc-2-(Hydroxymethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Compound MH3-3 (284.2mg, 0.8mmol) was dissolved in DMSO (5.0mL) was added TEA (0.2mL, 1.44mmol) and Compound S1-5 (259.5mg, 1.2mmol), microwave at 90 deg.] C of The reaction 12h, cooled to room temperature, dichloromethane (15 mL), then washed three times (15 mL), dried over anhydrous white solid was recrystallized from ethanol to give 243.8mg, 55.26%, 1030377-21-9

As the paragraph descriping shows that 1030377-21-9 is playing an increasingly important role.

Reference£º
Patent; Guangdong Zhong Hospital; Guangdong Experiment Animal Monitor Suo; Liu Bo; Xu Guangyu; Yu Jie; Wu Yue; Chen Cha; Xu Fangfang; Zhang Yu; Han Xiaodong; Lin Dongling; Huang Ren; Lu Jinjian; Zhang Yuqin; (62 pag.)CN106674254; (2017); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics