Day: September 27, 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.614730-97-1,1-Boc-4-Fluoro-4-(hydroxymethyl)piperidine,as a common compound, the synthetic route is as follows.

614730-97-1, Step B The product from Step A (1.44 g, 6.17 mmol) was dissolved in 6 ml of pyridine and the solution was cooled to 0C. p-Toluenesulfonyl chloride (1.29 g, 6.79 mmol) was added and the mixture was stirred at room temperature for 4 hours. The reaction mixture was diluted with dichloromethane (250 mL) and washed with water (50 mL). The organic phase was dried over Na2SO4, filtered and the solvent was removed. The residue was purified using a Biotage flash chromatography system (ethyl acetate/n-heptane: 20 to 50%) to give a yellowish oil (2.2 g, 92%). 1H-NMR (400 MHz, CDCl3): delta = 7.79 (d, 2H), 7.36 (d, 2H), 3.96 (brs, 2H), 3.03 (m, 2H), 2.46 (s, 3H), 1.80 (m, 2H), 1.63-1.49 (m, 4H), 1.47 (s, 9H)

614730-97-1 1-Boc-4-Fluoro-4-(hydroxymethyl)piperidine 22248400, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; AC Immune S.A.; EP2377860; (2011); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

503614-92-4, 1-(4-Methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylic acid is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

503614-92-4, 12.5 g (27.1 mmol) of substance of formula 11c obtained in example 10 is suspended in DMA, then under argon atmosphere 8.0 g (49.3 mmol) of carbonyldiimidazole (CDI) is added, and the mixture is heated to 60 C, and it is maintained at this temperature for 1 hour. Then 18.8 mL (13.7 g, 136 mmol) of triethylamine and 6.25 g (81 mmol) of ammonium acetate are added to the mixture. The stirring is continued for 1 hour. Water is added to the mixture and the suspension is slowly cooled to 20 C. The precipitated substance is filtered off and washed. After drying 11.36 g (24.7 mmol, 91%) of off-white substance is obtained. Mp.: 236-238 C.

The synthetic route of 503614-92-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; EGIS GYOGYSZERGYAR ZRT.; MRAVIK, Andras; NAGY, Tamas; FARAGO, Janos; VOLK, Balazs; LUKACS, Gyula; NEMETH, Gabor; CZOBORNE HATVARI, Ilona; SLEGEL, Peter; CSONKA-KIS, Gy?z?; KORMANY, Robert; (39 pag.)WO2016/20711; (2016); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.146093-46-1,4-(Aminoethyl)-1-N-Boc-piperidine,as a common compound, the synthetic route is as follows.

To a solution of 2-(4-oxo-3,4-dihydropyrido[3,4-d]pyrimidin-2-yl)benzofuran-7- carboxylic acid (1.0 eq) and 4-(2-Amino-ethyl)-piperidine-l -carboxylic acid tert-butyl ester (1.1 eq) in Nu,Nu-dimethylformamide were added N,N-diisopropylethylamine (2.0 eq) and HATU (1.2 eq). The mixture was allowed to stir for 30 min. It was diluted with brine and extracted with ethyl’ acetate twice. The combined organic extract was washed with brine twice and dried over magnesium sulfate (or extracted with UCT SPE CUBCX -cartr-idge)r4t- was concentrated- and- purified by combi-flashr~or~preparative^ HPLC., 146093-46-1

As the paragraph descriping shows that 146093-46-1 is playing an increasingly important role.

Reference£º
Patent; DONG-A SOCIO HOLDINGS CO., LTD.; KIM, Myeong-seop; PARK, Taesun; YOON, Taeyoung; YANG, Seung Min; KIM, Hae-Sun; KIM, Jun Gyu; (285 pag.)WO2016/68580; (2016); A2;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.214147-48-5,1-(4-Aminopiperidin-1-yl)ethanone hydrochloride,as a common compound, the synthetic route is as follows.

The sealed tube is charged with 7-bromo-5-chloroquinoxaline (50 mg; 0.21 mmol; 1.00 eq.), 1 -(4-aminopiperidin-1 -yl)ethan-1-one hydrochloride (38 mg; 0.27 mmol; 1.30 eq.), NaOtBu (59 mg; 0.62 mmol; 3.00 eqf.), BrettPhos Pd G1 (3.3 mg; 0.00 mmol; 0.02 eq.), BrettPhos (4.4 mg; 0.01 mmol; 0.04 eq.) and sealed with silicone PTFE coated cap. The air from the vessel is evacuated in vacuo thorough syringe and backfilled with argon. The cycle is repeated 3 times and anhydrous [1 ,4]-dioxane (1 .00 ml) is added thorough syringe. RM is heated and stirred for 1 h at 120C. Then RM is diluted with EtOAc and filtered through celite pad. Filtrate is evaporated resulted oily residue is purified by FCC (MeOH/DCM, gradient). 1-{4-[(8-Chloroquinoxalin- 6-yl)amino]piperidin-1-yl}ethan-1 -one (6.9 mg; 0.02 mmol; yield 10.4%;94% by UPLC) is obtained as brown glass.

214147-48-5, 214147-48-5 1-(4-Aminopiperidin-1-yl)ethanone hydrochloride 17221642, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; SELVITA S.A.; FABRITIUS, Charles-Henry Robert Yves; NOWAK, Mateusz Oktawian; WIKLIK, Katarzyna Anna; SABINIARZ, Aleksandra Barbara; BIE?, Marcin Dominik; BUDA, Anna Ma?gorzata; GUZIK, Pawel Szczepan; JAKUBIEC, Krzysztof Roman; MACIUSZEK, Monika; KWIECI?SKA, Katarzyna; TOMCZYK, Mateusz Micha?; GA??ZOWSKI, Micha? Miko?aj; GONDELA, Andrzej; DUDEK, ?ukasz Piotr; (681 pag.)WO2016/180536; (2016); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.287952-67-4,4-(4-Trifluoromethoxyphenoxy)piperidine,as a common compound, the synthetic route is as follows.

Example 25; Production of (5) -4- [4- (trifluoromethoxy) phenoxy] -l-{ 4- [ (2, 2, 4- trimethyl-1, 3-dioxolane-4-ly) methoxy] phenyl }piperidine; (S) -4- (4-Bromophenoxy)methyl-2, 2, 4-trimethyl-l, 3- dioxolane (2.32 g, 7.7 mmol), 4- [4-(trifluoromethoxy) phenoxy] piperidine (2.0 g, 7.7 mmol),tris (dibenzylideneacetone) dipalladium (0) (0.141 g, 0.15 mmol), 2- dicyclohexylphosphino-2′ – (N, N-dimethylamino) biphenyl (0.145 g, 0.37 mmol), potassium hydroxide (0.864 g, 15.4 mmol),tributylamine (5 mL) , and xylene (46 ml) were mixed, followed by stirring under a nitrogen atmosphere at 80 C for 8 hours. Using HPLC, it was confirmed that (S) -4- [4- (trifluoromethoxy) phenoxy] – l-{4- [ (2,2, 4-trimethyl-l, 3-dioxolane-4- ly) methoxy] phenyl }piperidine was produced with the inversion rate of 99%., 287952-67-4

Big data shows that 287952-67-4 is playing an increasingly important role.

Reference£º
Patent; OTSUKA PHARMACEUTICAL CO., LTD.; YAMAMOTO, Akihiro; SHINHAMA, Koichi; FUJITA, Nobuhisa; AKI, Shinji; OGASAWARA, Shin; UTSUMI, Naoto; WO2011/93529; (2011); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

22065-85-6, 1-Benzylpiperidine-4-carbaldehyde is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 20 Production of 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-ylidene]methylpiperidine using a mixed solvent of methanol and toluene and sodium hydroxide and adopting method A Into a 50-mL four-necked flask were charged 2.0 g (10.4 mmol) of 5,6-dimethoxy-1-indanone, 2.5 g (12.3 mmol, 1.2 equivalents) of 1-benzyl-4-formylpiperidine and 24 mL of a mixed solvent (methanol: toluene = 16: 14). After the air in the system was replaced with nitrogen, 0.5 g (12.5 mmol, 1.2 equivalents) of sodium hydroxide was added to the reaction solution with refluxing (65C). After completion of the addition, stirring was continued with refluxing for 1 hour to complete the reaction. Then, the reaction solution was air-cooled until crystals were precipitated. After the precipitation, the reaction solution was further cooled (cooling rate: 36C/hour) and the crystals precipitated at 4C or higher were collected by filtration. The crystals began to be precipitated at 49C. The crystals collected by filtration were washed with water (30 mL) and 6 mL of methanol and dried at 50C (drying time: 2 hours and 35 minutes) to obtain 3.31 g of the crystals of the title compound (yield: 84.3%). 1H-NMR data of these crystals agreed with those obtained in Example 1., 22065-85-6

22065-85-6 1-Benzylpiperidine-4-carbaldehyde 89584, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; Eisai R&D Management Co., Ltd.; EP1911745; (2008); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.216854-23-8,(S)-tert-Butyl piperidin-3-ylcarbamate,as a common compound, the synthetic route is as follows.

General procedure: A test tube equipped with a stir bar was charged with (S)-tert-butyl piperidin-3-ylcarbamate (205 mg, 1.02 mmol) and potassium carbonate (281 mg, 2.03 mmol). 1-(2-Bromoethyl)-2-fluorobenzene (170 muL, 1.22 mmol) and acetonitrile (3.0 mL) were added, and the mixture was heated in an 80 C oil bath. After heating overnight (~18 h), the reaction was partitioned between EtOAc and H2O, and the aqueous layer was extracted with EtOAc. The combined organics were concentrated under reduced pressure. The crude material was purified by silica gel chromatography (Rf in 60:40 hexanes:EtOAc = 0.24) to give the product as a colorless, viscous oil that slowly crystallized on standing (238 mg, 72%)., 216854-23-8

The synthetic route of 216854-23-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Hennessy, Edward J.; Saeh, Jamal C.; Sha, Li; MacIntyre, Terry; Wang, Haiyun; Larsen, Nicholas A.; Aquila, Brian M.; Ferguson, Andrew D.; Laing, Naomi M.; Omer, Charles A.; Bioorganic and Medicinal Chemistry Letters; vol. 22; 4; (2012); p. 1690 – 1694;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

3970-68-1, 4-Methylpiperidin-4-ol is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 7 4-Methyl-1-[3-[3-(trifluoromethyl)phenyl]sulfonyl-8-quinolyl]piperidin-4-ol Hydrochloride 4-Methylpiperidin-4-ol (292 mg, 2.53 mmol), 8-fluoro-3-(3-(trifluoromethyl)phenyl-sulfonyl)quinoline (200 mg, 0.563 mmol) and K2CO3 (311 mg, 2.252 mmol) were suspended in NMP (2 ml) and stirred in the Microwave at 225 C. for 35 min. The reaction mixture was diluted with ethyl acetate and washed 4* with water, dried and concentrated. The product was obtained by preparative HPLC chromatography on a reversed phase column. Finally the HCl salt was formed by adding one equivalent HCl to give 4-methyl-1-(3-(3-(trifluoromethyl)phenylsulfonyl)quinolin-8-yl)piperidin-4-ol hydrochloride (97 mg, yield 35.4%). LCMS (ESI+) m/z [M+H]+: 451.10 1H NMR (DMSO-d6, 500 MHz): delta=9.56 (d, J=2.1 Hz, 1H), 9.44 (d, J=2.1 Hz, 1H), 8.43-8.53 (m, 3H), 8.32 (d, J=8.2 Hz, 1H), 8.17 (d, J=7.9 Hz, 1H), 7.97 (t, J=7.9 Hz, 1H), 7.91 (t, J=7.9 Hz, 1H), 5.32-5.41 (m, broad, 1H), 4.04 (br s, 2H), 3.63 (s, 1H), 3.61 (s, 1H), 2.21 (m, 2H), 1.83 (m, 2H), 1.31 ppm (s, 3H)., 3970-68-1

The synthetic route of 3970-68-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Abbvie Deutschland GmbH & Co. KG; GENESTE, Herve; HAUPT, Andreas; POHLKI, Frauke; RELO, Ana Lucia; UNGER, Liliane; WICKE, Karsten; (53 pag.)US2017/260158; (2017); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.54012-73-6,Piperidin-3-amine,as a common compound, the synthetic route is as follows.

54012-73-6, In a sample bottle with stopper with a volume of 20 ml,1.00 g (10.0 mmol) of racemic 3-aminopiperidine,2.65 g (10.0 mmol) of N-p-toluyl-D-glutamic acid,5.55 g of methanol,And 0.97 g of water, and the mixture was heated to 60 C. for dissolution,10 mg of N-p-toluyl-D-glutamate of (S) -3-aminopiperidine was added.After cooling to 10 C.,After filtering the precipitated crystals,And dried to obtain 1.57 g of a salt.The optical purity of 3-aminopiperidine contained in the salt was 95.5% e. E. (S form).A portion of this salt was collected to quantify 3-aminopiperidine,The content rate is 27.5%This salt,It was confirmed to be a 1: 1 salt of 3-aminopiperidine and Np-toluyl-D-glutamic acid.Yield 43%.

The synthetic route of 54012-73-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; TORAY FINE CHEMICALS CO LTD; FUJINO, TOSHIHIRO; HIRAGA, HISAFUMI; (9 pag.)JP5838590; (2016); B2;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

4897-50-1,4897-50-1, 4-Piperidinopiperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of triphosgene (8 g, 26.9 mmol) in dry dichloromethane (40 mL) at -7 C were added dry triethylamine (1 mL, 7.1 mmol) and dropwise a solution of 1,4′-dipiperidine (5 g, 29.7 mmol) in dry dichloromethane (35 mL) over a period of 50 min. Then the solution was stirred at room temperature for 8 h, at which time the reaction was completed, the solution was filtered, the filtrate was concentrated, the residue was reacted with 23-hydroxybetulinic acid directly without further purification.

As the paragraph descriping shows that 4897-50-1 is playing an increasingly important role.

Reference£º
Article; Lan, Ping; Wang, Jiao; Zhang, Dong-Mei; Shu, Chang; Cao, Hui-Hui; Sun, Ping-Hua; Wu, Xiao-Ming; Ye, Wen-Cai; Chen, Wei-Min; European Journal of Medicinal Chemistry; vol. 46; 6; (2011); p. 2490 – 2502;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem