Category: 325145-35-5

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.325145-35-5,(S)-tert-Butyl 2-ethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a solution of 5-chloro-1- (chloromethyl) -2-methyl-3-nitrobenzene (D23 1.232 g) in DMF (20 mL) were added (S) -tert-butyl 2-ethylpiperazine-1-carboxylate (1 g) and K2CO3(1.935 g) at 60. After stirring overnight the mixture was poured into ice/water and then extracted with DCM (3×100 mL) . The combined organic layers were dried over Na2SO4 filtered and concentrated to give a yellow oil which was purified by column chromatography (eluting with EAPE5) to give the title compund (1.3 g) as a yellow solid. MS (ESI) C19H28ClN3O4requires 397 found 398 [M+H]+., 325145-35-5

The synthetic route of 325145-35-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; GLAXOSMITHKLINE (CHINA) R&D COMPANY LIMITED; LEI, Hui; MA, Xin; REN, Feng; LIN, Xichen; MARQUIS, Robert W., Jr.; WO2015/180614; (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.325145-35-5,(S)-tert-Butyl 2-ethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a solution of 5-chloro-1- (chloromethyl) -2-methyl-3-nitrobenzene (D23 1.232 g) in DMF (20 mL) were added (S) -tert-butyl 2-ethylpiperazine-1-carboxylate (1 g) and K2CO3(1.935 g) at 60. After stirring overnight the mixture was poured into ice/water and then extracted with DCM (3×100 mL) . The combined organic layers were dried over Na2SO4 filtered and concentrated to give a yellow oil which was purified by column chromatography (eluting with EAPE5) to give the title compund (1.3 g) as a yellow solid. MS (ESI) C19H28ClN3O4requires 397 found 398 [M+H]+., 325145-35-5

The synthetic route of 325145-35-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; GLAXOSMITHKLINE (CHINA) R&D COMPANY LIMITED; LEI, Hui; MA, Xin; REN, Feng; LIN, Xichen; MARQUIS, Robert W., Jr.; WO2015/180614; (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.325145-35-5,(S)-tert-Butyl 2-ethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a solution of 5-chloro-1- (chloromethyl) -2-methyl-3-nitrobenzene (D23 1.232 g) in DMF (20 mL) were added (S) -tert-butyl 2-ethylpiperazine-1-carboxylate (1 g) and K2CO3(1.935 g) at 60. After stirring overnight the mixture was poured into ice/water and then extracted with DCM (3×100 mL) . The combined organic layers were dried over Na2SO4 filtered and concentrated to give a yellow oil which was purified by column chromatography (eluting with EAPE5) to give the title compund (1.3 g) as a yellow solid. MS (ESI) C19H28ClN3O4requires 397 found 398 [M+H]+., 325145-35-5

The synthetic route of 325145-35-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; GLAXOSMITHKLINE (CHINA) R&D COMPANY LIMITED; LEI, Hui; MA, Xin; REN, Feng; LIN, Xichen; MARQUIS, Robert W., Jr.; WO2015/180614; (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.325145-35-5,(S)-tert-Butyl 2-ethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a solution of 5-chloro-1- (chloromethyl) -2-methyl-3-nitrobenzene (D23 1.232 g) in DMF (20 mL) were added (S) -tert-butyl 2-ethylpiperazine-1-carboxylate (1 g) and K2CO3(1.935 g) at 60. After stirring overnight the mixture was poured into ice/water and then extracted with DCM (3×100 mL) . The combined organic layers were dried over Na2SO4 filtered and concentrated to give a yellow oil which was purified by column chromatography (eluting with EAPE5) to give the title compund (1.3 g) as a yellow solid. MS (ESI) C19H28ClN3O4requires 397 found 398 [M+H]+., 325145-35-5

The synthetic route of 325145-35-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; GLAXOSMITHKLINE (CHINA) R&D COMPANY LIMITED; LEI, Hui; MA, Xin; REN, Feng; LIN, Xichen; MARQUIS, Robert W., Jr.; WO2015/180614; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

325145-35-5, (S)-tert-Butyl 2-ethylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

At 60 ° C (S) chloro-1- (chloromethyl) -2-methyl-3-nitrobenzene (D23, 1.232 g) in DMF (20 mL) was added (S)-2-ethylpiperazine-1-carboxylic acid tert-butyl ester(1 g) and K2CO3 (1.935 g). After taking a over night, The mixture is poured into ice / water,Then extracted with DCM (3 x 100 mL).The combined organic layers were dehydrated by Na2S04,Filter & apos; with concentrated to produce a yellow oil,Purification by column chromatography (using EpsilonAlpha: PE = 5percent) gave the title compound ( 3 g) as a yellow solid, 325145-35-5

Big data shows that 325145-35-5 is playing an increasingly important role.

Reference：
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; LEI, HUI; MA, XIN; REN, FENG; LIN, XICHEN; MARQUIS, ROBERT W., JR; (139 pag.)TW2017/14884; (2017); A;,
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.325145-35-5,(S)-tert-Butyl 2-ethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a solution of 5-chloro-1- (chloromethyl) -2-methyl-3-nitrobenzene (D23 1.232 g) in DMF (20 mL) were added (S) -tert-butyl 2-ethylpiperazine-1-carboxylate (1 g) and K2CO3(1.935 g) at 60. After stirring overnight the mixture was poured into ice/water and then extracted with DCM (3×100 mL) . The combined organic layers were dried over Na2SO4 filtered and concentrated to give a yellow oil which was purified by column chromatography (eluting with EAPE5) to give the title compund (1.3 g) as a yellow solid. MS (ESI) C19H28ClN3O4requires 397 found 398 [M+H]+., 325145-35-5

The synthetic route of 325145-35-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; GLAXOSMITHKLINE (CHINA) R&D COMPANY LIMITED; LEI, Hui; MA, Xin; REN, Feng; LIN, Xichen; MARQUIS, Robert W., Jr.; WO2015/180614; (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.325145-35-5,(S)-tert-Butyl 2-ethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a solution of 5-chloro-1- (chloromethyl) -2-methyl-3-nitrobenzene (D23 1.232 g) in DMF (20 mL) were added (S) -tert-butyl 2-ethylpiperazine-1-carboxylate (1 g) and K2CO3(1.935 g) at 60. After stirring overnight the mixture was poured into ice/water and then extracted with DCM (3×100 mL) . The combined organic layers were dried over Na2SO4 filtered and concentrated to give a yellow oil which was purified by column chromatography (eluting with EAPE5) to give the title compund (1.3 g) as a yellow solid. MS (ESI) C19H28ClN3O4requires 397 found 398 [M+H]+., 325145-35-5

The synthetic route of 325145-35-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; GLAXOSMITHKLINE (CHINA) R&D COMPANY LIMITED; LEI, Hui; MA, Xin; REN, Feng; LIN, Xichen; MARQUIS, Robert W., Jr.; WO2015/180614; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

325145-35-5, (S)-tert-Butyl 2-ethylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

1-(4-trifluoromethylbenzofur-7-yl)-3(S)-ethyl-4-tert-butoxycarbonylpiperazine Beginning with 1.45 gm (5.47 mMol) 4-trifluoromethyl-7-bromobenzofuran and 1.4 gm (6.53 mMol) 1-(tert-butoxycarbonyl)-2(S)-ethylpiperazine, 1.82 gm (84percent) of the desired compound were prepared essentially as described in Example 1. ESMS: m/e=399 (M+1)

325145-35-5, As the paragraph descriping shows that 325145-35-5 is playing an increasingly important role.

Reference：
Patent; Eli Lilly and Company; US6638936; (2003); B1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

325145-35-5, (S)-tert-Butyl 2-ethylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Chloride 3 (5.35 g, 24.4 mmol) was dissolved in DMF (50 mL, dried over molsieves). Piperazine 4 (5.0 g, 23.3 mmol) was added, followed by the addition of K2CO3 (8.0 gr, 58 mmol). The mixture was stirred overnight at 80°C. The DMF was evaporated under reduced pressure. The residue was dissolved in DCM (100 mL) and washed with water (50 mL). The organic layer was dried over Na2SO4, filtered and concentrated under vacuum to give crude Boc-protected product. This was dissolved in DCM (50 mL) and CF3COOH (5 mL) was added dropwise. The mixture was stirred for 1 hour at room temperature and subsequently concentrated under vacuum. The residue was dissolved in DCM (25 mL) and washed with 1.0M aq. NaOH (25 mL) and water (25 mL). The organic layer was dried over Na2SO4, filtered and concentrated under vacuum. Column chromatography (gradient: EtOAc/Et3N 99/1 toEtOAc/MeOH/Et3N 80/20/1) afforded the product as a white solid (3.35 g, 46 percent).LC-MS purity: 98+ percent. 1H-NMR (CDCl3, 400 MHz) delta 8.48 (d, 1H, J=2.1 Hz), 7.97 (d, 1H, J=2.1Hz), 6.09 (br t, 1H), 4.00-3.89 (m, 2H), 3.48 (dq, 2H, J1=7.3 Hz), 3.11-2.89 (m, 3H), 2.82-2.72(m, 1H), 2.58 (dd, 1H, J1=12.4 Hz, J2=10.0 Hz), 1.52-1.35 (m, 2H), 1.23 (t, 3H, J=7.3 Hz),0.97 (t, 3H, J=7.5 Hz).

325145-35-5, The synthetic route of 325145-35-5 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Scholten, Danny J.; Roumen, Luc; Wijtmans, Maikel; Verkade-Vreeker, Marlies C. A.; Custers, Hans; Lai, Michael; De Hooge, Daniela; Canals, Meritxell; De Esch, Iwan J. P.; Smit, Martine J.; De Graaf, Chris; Leurs, Rob; Molecular Pharmacology; vol. 85; 1; (2014); p. 116 – 126;,
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.325145-35-5,(S)-tert-Butyl 2-ethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

ER-895473 (103 mg, 0.261 mmol, 27.1percent yield) was prepared in a similar manner to ER-899742 starting with 38 (286 mg, 0.962 mmol) and (S)-tert-butyl 2-ethylpiperazine-1-carboxylate (206 mg, 0.962 mmol). DMF (3 mL) was used instead of DCM for the amide forming reaction and 2.0 M HCl in ethyl ether (1.3 mL, 2.6 mmol) was used in the Boc-deprotection process using acetonitrile (1 mL) as a solvent. ER-895473 was purified by reverse-phase HPLC (X-Bridge C18 19×100 mm column; eluting with a gradient of increasing acetonitrile in water containing 0.1percent formic acid). The product fractions were combined and concentrated to dry followed by dilution in MeOH (1 mL), passed through as basic silica gel plug (Biotage SiCO3, 1 g, eluting with MeOH (1 mL)), concentrated and dried in vacuo.To a stirred solution of 38 (300 mg, 1.01 mmol) in DCM (2 mL) was added the mixture of (3S,4R)-tert-butyl 3-amino-4-fluoropyrrolidine-1-carboxylate and (3R,4S)-tert-butyl 3-amino-4-fluoropyrrolidine-1-carboxylate, 77 (205.3 mg, 1.005 mmol), HBTU (247 mg, 1.211 mmol) and DIEA (0.70 mL, 4.04 mmol) followed by stifling at rt for 16 h. The was found complete and concentrated to dryness followed by dissolving in EtOAc (20 mL), washed 1 time with water (10 mL), 2 N citric acid in water (10 mL), saturated NaHCO3 (10 mL), and brine (10 mL). The combined aqueous layers were extracted 3 times with EtOAc (10 mL ea.) after which time the combined organic fractions were dried over MgSO4, filtered and concentrated to dry. The crude product was purified over a 25 g Biotage silica gel column eluting with 0-10percent MeOH in DCM (200 mL total) to provide the diastereomeric mixture of 78 and 79., 325145-35-5

Big data shows that 325145-35-5 is playing an increasingly important role.

Reference：
Patent; CARLSON, ERIC; HANSEN, HANS; HAWKINS, LYNN; ISHIZAKA, SALLY; MACKEY, MATTHEW; SCHILLER, SHAWN; OGAWA, CHIKAKO; DAVIS, HEATHER; US2015/105370; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics