Tag: M.W:200-300

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.154590-35-9,tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

A solution of the product of EXAMPLE 13A (70 mg, 0.21 mmol), tert-butyl 4-(4-amino-2-fluorophenyl)pip- erazine-1 -carboxylate (61 mg, 0.21 mmol) and catalytic p-toluenesulfonic acid (5mg) inn-butanol (3 mL) was heated100C. for 18 hours. After cooling to ambient temperature, the mixture was poured into saturated aqueous sodium bicarbonate (50 mL). The resulting solution was extracted with ethyl acetate (3×30 mL), and the organic layers were combined, dried over anhydrous sodium sulfate, filtered and concentrated. The residue was purified by preparative thin layer chromatography using 20:1 dichloromethane/methanol to afford the crude title compound which was used in the next step without further purification. MS: 598 (M+Hj., 154590-35-9

154590-35-9 tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate 16203630, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; ABBVIE INC.; Vasudevan, Anil; Penning, Thomas Dale; Chen, Huanming; Liang, Bo; Wang, Shaohui; Zhao, Zhongqiang; Chai, Dikun; Yang, Leifu; Gao, Yingxiang; Pliushchev, Marina; US2014/171429; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

694499-26-8,694499-26-8, 4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

3-lodo-4-methylbenzoyl chloride (0.48 g, 1.7 mmol), prepared from the reaction of 3-iodo-4-methylbenzoic acid and SOCI2 (as previously described), was added to a solution of 4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (0.47 g, 1.7 mmol), lambda/./V- diisopropylethylami?e (0.26 g, 2.0 mmol), and a catalytic amount of DMAP in THF (10 mL). After stirring at rt for 2 h, the reaction was quenched with water. EtOAc was added and the layers separated. The combined organic layers were concentrated to dryness and purified by silica gel chromatography (eluted with 5% MeOH/DCM, MeOH was pre-saturated with ammonia gas), to provide 0.51 g of product as an off-white solid.

The synthetic route of 694499-26-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ARIAD PHARMACEUTICALS, INC.; WO2007/75869; (2007); 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.122833-04-9,2-Methoxy-4-(4-methylpiperazin-1-yl)aniline,as a common compound, the synthetic route is as follows.

General procedure: General procedure for the synthesis of 15b-15u. To a solution ofcompound 13a (0.41 g, 1.06 mmol) in 2-butanol (5 mL), 1-(2-(dimethylamino)ethyl)-1H-pyrazol-4-amine (0.196 g, 1.27 mmol)and trifluoroacetic acid (94 mL) were added in a sealed tube. Thereactionwas heated at 95 C for 18 h. The reaction mixturewas thenallowed to cool to room temperature. The mixture was transferredto a round-bottom flask and then the solvent was removed underreduced pressure. The residue was dissolved in DCM (2.0 mL) andTFA (2.0 mL), and the resulting mixture was stirred for 5 h at roomtemperature. The solvent was removed under reduced pressure,and the residue was neutralized with saturated NaHCO3 aqueoussolution. The water layer was extracted with DCM. The organiclayer was combined and washed with brine, dried over Na2SO4,filtered, concentrated, and purified by silica gel chromatography toafford 15a as a yellow solid (0.264 g, 65% for two steps).

122833-04-9, As the paragraph descriping shows that 122833-04-9 is playing an increasingly important role.

Reference：
Article; Yu, Lei; Huang, Minhao; Xu, Tianfeng; Tong, Linjiang; Yan, Xiao-e; Zhang, Zhang; Xu, Yong; Yun, Caihong; Xie, Hua; Ding, Ke; Lu, Xiaoyun; European Journal of Medicinal Chemistry; vol. 126; (2017); p. 1107 – 1117;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

694499-26-8, 4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

4-(4-methylpiperazin-1-ylmethyl)-3-trifluoromethylaniline (2.27 g, 8.3 mmol), 3-iodo-4-methyl-benzoyl chloride (10 mmol), 15 ml tetrahydrofuran, and 10 ml triethylamine were added into a reactor and stirred at room temperature for 4 hours. After completion of the reaction, the resultant was washed with a saturated NaHCO3 solution, extracted with ethyl acetate and water, washed with a saturated NaCl solution, dried over anhydrous Na2SO4. The solvent was removed by distillation under reduced pressure. The residue was purified by silica gel column chromatography, to give a yellow oily matter. 1H NMR (500 MHz, CDCl3) delta: 8.39 (s, 1H, N-H), 8.29 (s, 1H, Ar-H), 7.88 (d, 1H, Ar-H), 7.86 (s, 1H, Ar-H), 7.75 (d, 1H, Ar-H), 7.73 (d, 1H, Ar-H), 7.28 (d, 1H, Ar-H), 3.62 (s, 2H, PhCH2), 2.60 (b, 8H, 4*-CH2), 2.47 (s, 3H, -CH3), 2.31 (s, 3H, -CH3)., 694499-26-8

As the paragraph descriping shows that 694499-26-8 is playing an increasingly important role.

Reference：
Patent; Nanjing Sanhome Pharmaceutical Co., Ltd.; Wang, Yong; Zhao, Liwen; Zhang, Wenping; Chen, Hongyan; Bi, Sheng; Gao, Yiping; Chen, Hongbin; Liu, Yang; Xu, Xin; Zhang, Cang; US2015/152088; (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.278788-66-2,(R)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step D: (3S,9aR}-3-(3-Cyano-4-fluoro-2-methyl-phenyl)-3-hydroxy-hexahydro-pyrazino[2,1-c][1,4]oxazine-8-carboxylic acid tert-butyl ester: Diisopropylethylarnine (44.0 mL, 252 mmol)was added to a stirred, room temperature mixture of72 wt% 3-(2-Bromo-acetyl)-6-fluoro-2-methyl-benzonitrile (69 g, 194 mmol) and (R)-4-N-Boc-2-hydroxymethyl-piperazine ( 42.0 g, 194 mmol) in THF (1000 mL) and the mixture was stirred at room temperature for 18h. The reactionwas diluted with 1 L EtOAc, washed 2x with 500 mL 10% w/wNaHC03 aqueous solution,dried over MgS04, filtered and concentrated. The residue was purified by column chromatographyon silica gel ( 40-80% EtOAc/Hexanes, linear gradient), to give the title compound.?~+%, 278788-66-2

The synthetic route of 278788-66-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; MERCK SHARP & DOHME CORP.; PASTERNAK, Alexander; BLIZZARD, Timothy; CHOBANIAN, Harry; DE JESUS, Reynalda; DING, Fa-Xiang; DONG, Shuzhi; GUDE, Candido; KIM, Dooseop; TANG, Haifeng; WALSH, Shawn; PIO, Barbara; JIANG, Jinlong; WO2013/28474; (2013); 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.161357-89-7,1-(Methylsulfonyl)piperazine hydrochloride,as a common compound, the synthetic route is as follows.

2-Chloro-4-morpholinofuro[3,2-d]pyrimidine-6-carbaldehyde 39 prepared following Example 20 (65 mg, 1.0 eq) was dissolved in 1 ,2-dichloroethane (9.7 ml) and treated with hydrochloride salt of 1-methanesulfonylpiperazine (69 mg, 1.4 eq), sodium acetate (28 mg, 1.4 eq) and trimethyl orthoformate (0.27 ml, 10 eq). Reaction mixture was stirred at r.t. for 12 h. Sodium triacetoxyborohydride (62 mg, 1.2 eq) was added and reaction mixture was stirred at r.t. for 8 h. Reaction mixture was quenched with saturated aq. NaHCO3 and extracted with dichloromethane. The combined organic layers were dried (Na2SO4) and concentrated. The crude reaction mixture was purified by flash chromatography to yield 2- chloro-6-((4-(methylsulfonyl)piperazin- 1 -yl)methyl)-4-morpholmofuro [3 ,2-d]pyrimidine(70 mg, 68%) : MS (Ql) 416 (M)+., 161357-89-7

161357-89-7 1-(Methylsulfonyl)piperazine hydrochloride 16265612, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; PIRAMED LIMITED; GENENTECH, INC.; BAYLISS, Tracy; CHUCKOWREE, Irina; FOLKES, Adrian; OXENFORD, Sally; WAN, Nan, Chi; CASTANEDO, Georgette; GOLDSMITH, Richard; GUNZNER, Janet; HEFFRON, Tim; MATHIEU, Simon; OLIVERO, Alan; STABEN, Steven; SUTHERLIN, Daniel, P.; ZHU, Bing-Yan; WO2008/70740; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

129799-15-1, Methyl 1-Boc-piperazine-2-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

129799-15-1, EXAMPLE 20 Preparation of 1-tert-butyl 2-methyl 4-(4-chlorophthalazin-1-yl)piperazine-1,2-dicarboxylate (JK-16) 1,4-dichlorophthalazine (741 mg, 3.72 mmol), 1-tert-butyl 2-methyl piperazine-1,2-dicarboxylate (1.00 g, 4.09 mmol), N,N-diisopropylethylamine (0.972 mL), and 4-methyl-2-pentanone (6 mL) were heated at 120 for 16 hours. The solvent was removed and the residue purified by chromatography over silica using a gradient of hexanes/0-70% ethyl acetate. The compound was obtained as a white solid. MS (M+H)+=407.1.

129799-15-1 Methyl 1-Boc-piperazine-2-carboxylate 2756818, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Amgen Inc.; US2009/48259; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

192130-34-0, tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 48; 4-{2-[5-(3-Trifluoromethoxy-phenyl)-imidazo[2,1-b][1 ,3,4]thiadiazol-2- ylamino]-ethyl}-piperazine-1-carboxylic acid tert-butyl ester; A mixture of 2-methanesulfonyl-5-(3-trifluoromethoxy-phenyl)-imidazo[2, 1- b][1 ,3,4]thiadiazole (1 16 mg, 0.319 mmol), 4-N-(2-aminoethyl)-1 -N-boc- piperazine (1 10 mg, 0.479 mmol) and Et3N (0.089 mL, 0.639 mmol) in ‘PrOH (5 mL) was heated in a sealed tube at 1 10°C for 16 hours. On cooling, DCM was added and the mixture was washed with H20. The organic layer was dried (sodium sulfate), filtered and concentrated. The residue was purified by column chromatography (Isolute/Flash, Sill, 0percent to 20percent MeOH in DCM) to give the desired product (4-{2-[5-(3-trifluoromethoxy-phenyl)-imidazo[2, 1 – b][1 ,3,4]thiadiazol-2-ylamino]-ethyl}-piperazine-1 -carboxylic acid tert-butyl ester) (20 mg, 12percent yield).HPLC-MS (method 1): Rt= 3.99 min, [M+1f m/z 513.2.H NMR (300 MHz, MeOD) delta 8.04 (s, 1 H), 7.90 (m, 1 H), 7.52 (s, 1 H), 7.51 (t, J = 8.1 Hz, 1 H), 7.19 (m, 1 H), 3.62 (t, J = 6.4 Hz, 2H), 3.44 (m, 4H), 2.72 (t, J = 6.4 Hz, 2H), 2.54 (m, 4H), 1.46 (s, 9H).

192130-34-0, As the paragraph descriping shows that 192130-34-0 is playing an increasingly important role.

Reference：
Patent; CENTRO NACIONAL DE INVESTIGACIONES ONCOLOGICAS (CNIO); PASTOR FERNANDEZ, Joaquin; GARCIA COLLAZO, Ana, Maria; NOYA MARINO, Beatriz; GONZALEZ CANTALAPIEDRA, Esther; WO2012/20217; (2012); 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.262368-30-9,N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide,as a common compound, the synthetic route is as follows.

Method 2; A suspension of methyl-3-[methoxy(phenyl)methylene]-2-oxoindoline-6- carboxylate (20,0 g; 0,064 mol) and N-(4-aminophenyl)-N-methyl-2-(4- methylpiperazin-1-yl)acetamide (17,1 g; 0,065 mol) in methanol (180 ml) is heated to reflux for 7,5 h. The resulting suspension is cooled down to 10 0C within 1 h and stirring is maintained for 1 h. After filtration, the solid is washed with ice cold methanol (80 ml) and dried to afford 31 ,0 g (89,0 %) of the “anilino” compound as yellow crystals., 262368-30-9

262368-30-9 N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide 21927707, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; WO2009/71523; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics