New learning discoveries about 161357-89-7

161357-89-7, As the paragraph descriping shows that 161357-89-7 is playing an increasingly important role.

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.

To a suspension of Example 1285A (0.091 g, 0.21 1 mmol) and l-(methylsulfonyl)piperazine hydrochloride (0.057 g, 0.284 mmol) in 1,4-dioxane (1 mL), N-ethyl-N-isopropylpropan-2-amine (0.2 mL, 1.145 mmol) was added. The mixture was stirred for 72 hours at room temperature. The solvent was removed and the product was purified by flash chromatography on silica gel (AnaLogix IntelliFlash) eluting with a gradient of 0-50% ethyl acetate in heptanes to afford the title compound. MS (ESI+) m/z: 40.3.8 (M+H)+.

161357-89-7, As the paragraph descriping shows that 161357-89-7 is playing an increasingly important role.

Reference:
Patent; ABBVIE INC.; ABBVIE PHARMACEUTICAL TRADING (SHANGHAI) CO., LTD.; TONG, Yunsong; BRUNCKO, Milan; CLARK, Richard F.; CURTIN, Michael L.; FLORJANCIC, Alan S.; FREY, Robin R.; GONG, Jianchun; HANSEN, Todd M.; JI, Zhiqin; LAI, Chunqiu; MASTRACCHIO, Anthony; MICHAELIDES, Michael; MIYASHIRO, Juliem; RISI, Roberto M.; SONG, Xiaohong; TAO, Zhi-fu; WOODS, Keith W.; ZHU, Guidong; PENNING, Thomas; SOUERS, Andrew; GOSWAMI, Rajeev; IQUTURI, Omprakash Reddy; DABBEERU, Madhu Babu; WO2014/139328; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

New learning discoveries about 1-(Methylsulfonyl)piperazine hydrochloride

161357-89-7, As the paragraph descriping shows that 161357-89-7 is playing an increasingly important role.

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.

4-[5-(4-Methanesulfonyl-piperazin-1 -yl)-2-methyl-2,3-dihydro-furo[2,3-clpyridin-2-yl1- piperidine-1 -carboxylic acid tert-butyl ester4-(5-Chloro-2-methyl-2,3-dihydro-furo[2,3-c]pyridin-2-yl)-piperidine-1 -carboxylic acid tert-butyl ester (100 mg) is added to a mixture of 1 -(methylsulfonyl)piperazine hydrochloride (70 mg), Pd2(dba)3 (65 mg), Xantphos (123 mg), and potassium tert- butylate (75 mg) in toluene (4 mL) under an argon atmosphere. The reaction mixture is stirred in an oil bath at 105C over night. After cooling to room temperature water is added and the mixture is extracted with ethyl acetate. The combined extracts are concentrated in vacuo and the residue is chromatographed on silica gel(cyclohexane/ethyl acetate 50:50? 0: 100) to give the title compound. LC (method 1 1 ): tR = 1 .03 min; Mass spectrum (EST): m/z = 481 [M+H]+.

161357-89-7, As the paragraph descriping shows that 161357-89-7 is playing an increasingly important role.

Reference:
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; HIMMELSBACH, Frank; ECKHARDT, Matthias; HEINE, Niklas; LANGKOPF, Elke; NOSSE, Bernd; WO2012/80476; (2012); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Simple exploration of 1-(Methylsulfonyl)piperazine hydrochloride

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

161357-89-7, 1-(Methylsulfonyl)piperazine hydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred solution of intermediate 6 (200 mg, 0.53 mmol ) and 1-(methylsulfonyl)piperazine hydrochloride (87 mg, 0.53 mmol) in dry toluene (5 ml_), sodium tert butoxide (150 mg, 1.6 mmol) was added at RT and the resulting solution was flushed with nitrogen for 10 min. BINAP (66 mg, 0.1 mmol), Pd (dba (98 mg, 0.1 mmol) were added and the reaction mixture was flushed again with nitrogen for 10 min. It was then stirred at 100 C overnight. After completion of the reaction, the reaction mixture was diluted with EtOAc (20 mL) and filtered through celite pad. The filtrate was concentrated under vacuum and resulting crude product was purified by flash chromatography (Eluent: 47% EtOAC in pet ether) to afford the title compound. Yield: 5% (1 1 .3 mg, off-white solid). 1H NMR (400 MHz, DMSO-cfe): d 7.09 (d, J = 8.4 Hz, 2H), 6.92-6.90 (m, 3H), 6.85 (d, J = 2.0 Hz, 1 H), 6.82-6.80 (m, 1 H), 4.22 (s, 4H), 3.61 (d, J = 12.8 Hz, 1 H), 3.23-3.20 (m, 10H), 2.92 (s, 3H), 2.1 1 -2.06 (m, 2H), 1.72-1.68 (m, 2H), 1.56-1.48 (m, 1 H). LCMS: (Method A) 458.1 (M +H), Rt.1.570 min, 99.4% (Max). HPLC: (Method A) Rt. 3.038 min, 99.5% (Max), 99.4% (220 nm).

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

Reference:
Patent; ASCENEURON S. A.; QUATTROPANI, Anna; WISHART, Grant; KULKARNI, Santosh S.; RAKESH, Paul; (338 pag.)WO2020/39027; (2020); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Some tips on 1-(Methylsulfonyl)piperazine hydrochloride

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

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

New learning discoveries about 1-(Methylsulfonyl)piperazine hydrochloride

As the paragraph descriping shows that 161357-89-7 is playing an increasingly important role.

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.

A -mixture of 4,6-dichloropyrinidine (39.4 g), 1-mesylpiperazine hydrochloride (55.7 g) and triethylamine (116 ml) in ethanol (500 ml) was stirred at reflux temperature for 4 hours. The mixture was then stirred at room temperature for 12 hours. The solid, which had separated, was collected by filtration, slurry washed with ethanol (2×80 ml 160 ml) then with diethyl ether (150 ml), and dried to give 1-(6-chloropyrimidin-4-yl)4-mesylpiperazine as a cream solid (71.9 g). mp 200-202 C. [00257] NMR (d6-DMSO): 2.88 (s, 3H), 3.18 (m, 4H), 3.80 (m, 4H), 7.04 (s, 1H), 8.38 (m, 1H); m/z 277.3 (M+1)., 161357-89-7

As the paragraph descriping shows that 161357-89-7 is playing an increasingly important role.

Reference:
Patent; AstraZeneca AB; US6734184; (2004); B1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Brief introduction of 161357-89-7

The synthetic route of 161357-89-7 has been constantly updated, and we look forward to future research findings.

161357-89-7, 1-(Methylsulfonyl)piperazine hydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 15 1 -mesyl-4-(5-methoxycarbonyl-2-pyridyl)piperazine 1-Mesylpiperazine hydrochloride (4.24 g) was added to a solution of methyl 6-chloronicotinate (1.7 g) and N,N-diisopropylethylamine (6.3 ml) in dimethylacetamide (20 ml) and the mixture was heated at 120 C. for 2 hours.. The mixture was allowed to cool to ambient temperature and poured onto crushed ice/water (50 ml) to precipitate a tan solid.. The solid was collected by filtration and dried at 80 C. for 18 hours in a vacuum oven, to give 1-mesyl-4-(5-methoxycarbonyl-2-pyridyl)piperazine (2.05 g), mp 205-207 C. NMR (d6-DMSO): 2.90 (s, 3H), 3.20 (m, 4H), 3.78 (m, 3H), 3.80 (s, 3H), 6.92 (d, 1H), 8.00 (dd, 1H), 8.67 (d, 1H), m/z 300 (M+1)., 161357-89-7

The synthetic route of 161357-89-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; AstraZeneca AB; US6734184; (2004); B1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Brief introduction of 161357-89-7

The synthetic route of 161357-89-7 has been constantly updated, and we look forward to future research findings.

161357-89-7, 1-(Methylsulfonyl)piperazine hydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

4-(5-Chloro-2-methyl-2,3-dihydro-furo[2,3-c]pyridin-2-yl)-piperidine-1-carboxylic acid tert-butyl ester (100 mg) is added to a mixture of 1-(methylsulfonyl)piperazine hydrochloride (70 mg), Pd2(dba)3 (65 mg), Xantphos (123 mg), and potassium tert-butylate (75 mg) in toluene (4 mL) under an argon atmosphere. The reaction mixture is stirred in an oil bath at 105 C. over night. After cooling to room temperature water is added and the mixture is extracted with ethyl acetate. The combined extracts are concentrated in vacuo and the residue is chromatographed on silica gel (cyclohexane/ethyl acetate 50:50?0:100) to give the title compound. LC (method 1): tR=1.03 min; Mass spectrum (ESI+): m/z=481 [M+H]+., 161357-89-7

The synthetic route of 161357-89-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; US2012/322784; (2012); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Simple exploration of 161357-89-7

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

161357-89-7, 1-(Methylsulfonyl)piperazine hydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 5 This Example illustrates the preparation of (R or S) N- (3- [4- methanesulphonylpiperazinyl]-3-phenylpropyl)-4- [2- (4-fluorophenylsulphonyl) ethyl] – piperidine (Compound 14, Table III). A solution of (R or S) N- (3-chloro-3-phenylpropyl)-4- [2- (4-fluorophenylsulphonyl)- ethyl] -piperidine (Method F; 310 mg) in dichloromethane (6 ml) was added to N- methanesulphonyl-piperazine hydrochloride (150 mg) followed by triethylamine (313)-D). The mixture was stirred for 48 hours, diluted with dichloromethane (5 ml) and MP-carbonate resin (1.34g), PS-ISOCYANATE resin (682 mg) and PS-thiophenol resin (577 mg) were added. The mixture was stirred for 5 hours, filtered and the resins were washed with 10% methanol in dichloromethane (2×25 ml). The combined filtrates were evaporated to dryness and the residue was passed through a 20g Isolute column eluted with a solvent gradient of ethyl acetate-10% methanol/ethyl acetate to give the title compound, yield 81 mg; MH+ 552. NMR (CDCL3) : 1.12-1. 32 (m, 4H), 1.52-1. 66 (m, 4H), 1.76-1. 93 (m, 3H), 2.08 (m, 1H), 2.21 (m, 1H), 2.47-2. 51 (m, 4H), 2.71 (s, 3H), 2.77-2. 88 (m, 2H), 3.03-3. 10 (m, 2H), 3.12-3. 21 (m, 4H), 3.37 (m, 1H), 7.14 (d, 2H), 7.15-7. 32 (m, 5H), 7.88 (m, 2H)., 161357-89-7

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

Reference£º
Patent; ASTRAZENECA AB; WO2004/56773; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Analyzing the synthesis route of 161357-89-7

The synthetic route of 161357-89-7 has been constantly updated, and we look forward to future research findings.

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.

Example 5: . 2-(lH-IndoI-4-yI)-6-(4-inethanesuIfonvI-piperazin-l-vImethvI)-4- morphoIm-4-yI-thienor2,3-d1pyrimidine; 2-Chloro-6-(4-methyl-piperazm-l-ylmethyl)-4-morpholin-4-yl-thieno[2,3- dlpyrimidine ‘ 2-Chloro-4-morpholin-4-yl-thieno[2,3-d]pyrimidine-6-carbaldehyde (400 mg) and 1-methanesulfonyl-piperazine hydrochloride (1.3eq.) were stirred together in dry 1,2-dichloroethane (20 mL). After 4h sodium triacetoxyborohydride (2.3 eq.) was added and the mixture stirred overnight. The mixture was diluted with Na2CO3 solution then extracted with ethyl acetate. Combined extracts were dried (Na2SO4), filtered and concentrated. Trituration gave product (60%)., 161357-89-7

The synthetic route of 161357-89-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PIRAMED LIMITED; WO2007/122410; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Analyzing the synthesis route of 161357-89-7

The synthetic route of 161357-89-7 has been constantly updated, and we look forward to future research findings.

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.

A suspension of (3R,4S)-1-benzyl-4-(4-bromophenyl)-N,N-dimethylpyrrolidin-3-amine (3.24 g, 9.02 mmol), 1-(methylsulfonyl)piperazine hydrochloride (2.172 g, 10.82 mmol), tris(dibenzylideneacetone)dipalladium (0) (0.826 g, 0.902 mmol), 2-(dicyclohexylphosphine)-2′,4′,6′-tri-isopropylbiphenyl (0.860 g, 1.803 mmol) and sodium tert-butoxide (2.167 g, 22.54 mmol) in dioxane (32.2 ml) in a 250 ml round bottom flask was taken through three vacuum/nitrogen-purge cycles and heated in a heating block under a condenser at 110C for 2 hours. The mixture was diluted with ethyl acetate and filtered through diatomaceous earth with ethyl acetate washes. The filtrate was washed with saturated sodium bicarbonate (20 ml), dried with magnesium sulfate, filtered, and concentrated. The residue was flash chromatographed (50 mm silica gel column; 6.5% methanol/dichloromethane w/0.1% ammonium hydroxide) to afford the title compound., 161357-89-7

The synthetic route of 161357-89-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Curtin, Michael L.; Pliushchev, Marina A.; Li, Huan-Qiu; Torrent, Maricel; Dietrich, Justin D.; Jakob, Clarissa G.; Zhu, Haizhong; Zhao, Hongyu; Wang, Ying; Ji, Zhiqin; Clark, Richard F.; Sarris, Kathy A.; Selvaraju, Sujatha; Shaw, Bailin; Algire, Mikkel A.; He, Yupeng; Richardson, Paul L.; Sweis, Ramzi F.; Sun, Chaohong; Chiang, Gary G.; Michaelides, Michael R.; Bioorganic and Medicinal Chemistry Letters; vol. 27; 7; (2017); p. 1576 – 1583;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics