Day: September 11, 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.336191-17-4,tert-Butyl 2,8-diazaspiro[4.5]decane-2-carboxylate,as a common compound, the synthetic route is as follows.

[00139] Step 1) A mixture of tert-butyl 2,8-diazaspiro[4.5]decane-2-carboxylate (Intermediate 10, 1.00 g, 4.16 mmol), 4-fluoropyridine hydrochloride (Intermediate 15, 614 mg, 4.60 mmol) and K2CO3 (1.74 g, 12.6 mmol) in MeCN (80 mL) was heated at 80C overnight before cooling to rt and concentration in vacuo. The residue was partitioned between EtOAc and H2O, the organic phase was washed with brine, dried (MgSO4), and concentrated in vacuo. (0324) Purification by gradient flash chromatography, eluting with 0-100% solvent B in DCM (where solvent B is 7N NH3 in MeOH / DCM, 1:9) yielded tert-butyl 8-(pyridin-4-yl)-2,8- diazaspiro[4.5]decane-2-carboxylate (610 mg, 1.92 mmol) as a brown, viscous oil. (0325) LCMS (Method B): m/z 318.2 (ES+), at 1.36 min. (0326) 1H NMR: (400 MHz, CD3OD) delta: 1.46 (s, 9H), 1.63-1.68 (m, 4H), 1.81-1.85 (m, 2H), 3.23 (s 2H), 3.36-3.54 (m, 6H), 6.82-6.83 (m, 2H), 8.07-8.09 (m, 2H)., 336191-17-4

As the paragraph descriping shows that 336191-17-4 is playing an increasingly important role.

Reference£º
Patent; HEPTARES THERAPEUTICS LIMITED; BUCKNELL, Sarah Joanne; CHRISTOPHER, John Andrew; CONGREVE, Miles Stuart; DEFLORIAN, Francesca; PICKWORTH, Mark; MASON, Jonathan Stephen; (201 pag.)WO2018/178938; (2018); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

657-36-3, 4-Trifluoromethylpiperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,657-36-3

General procedure: To a stirred solution of compound 7 (200 mg, 0.87 mmol) in DCM (10 mL) was added amines (1.0 mmol), EDC(186 mg, 1.2 mmol), and HOBt (153 mg, 1.2 mmol) at room temperature. The mixture was stirred for 3 hrs, quenchedby H2O (15 mL), and extracted by DCM (15 mL ¡Á 3). The organic layer was dried over anhydrous MgSO4, filtered,and concentrated. The residue was purified by chromatography on a silica gel column to afford compound 8a-l as acolorless oil.

As the paragraph descriping shows that 657-36-3 is playing an increasingly important role.

Reference£º
Article; Lv, Kai; Tao, Zeyu; Liu, Qian; Yang, Lu; Wang, Bin; Wu, Shuo; Wang, Apeng; Huang, Menghao; Liu, Mingliang; Lu, Yu; European Journal of Medicinal Chemistry; vol. 151; (2018); p. 1 – 8;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.163271-08-7,tert-Butyl (4-methylpiperidin-4-yl)carbamate,as a common compound, the synthetic route is as follows.,163271-08-7

Preparation of tert-butyl (l-(5-(3-cvano-6-hydroxypyrazolorL5-a1pyridin- 4-yl)pyridin-2-yl)-4-methylpiperidin-4-yl)carbamate. To a solution of 4-(6-fluoropyridin-3- yl)-6-hydroxypyrazolo[l,5-a]pyridine-3-carbonitrile (Intermediate P66; 3.0 g, 9.44 mmol) and tert-butyl 4-methylpiperidin-4-ylcarbamate (2.83 mg, 13.2 mmol) in DMSO (12 mL) was added DIEA (4.93 mL, 28.3 mmol). The reaction was stirred 16 h at 90C. After cooling to ambient temperature, the reaction mixture was diluted into water and acidified to pH 5 using a 10% citric acid solution and stirred for 15 min at ambient temperature. The suspension was filtered and the precipitate was rinsed with water. The isolated solids were dissolved in 4: 1 DCM:IPA and dried over anhydrous Na2S04(S), filtered and concentrated in vacuo. The residue was purified using silica chromatography (5-75% EtOAc in DCM) to afford the title compound (assumed theoretical yield, 4.23 g) in sufficient purity for step 2. MS (apci) m/z= 449.3 (M+H)

The synthetic route of 163271-08-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ANDREWS, Steven W.; ARONOW, Sean; BLAKE, James F.; BRANDHUBER, Barbara J.; COLLIER, James; COOK, Adam; HAAS, Julia; JIANG, Yutong; KOLAKOWSKI, Gabrielle R.; MCFADDIN, Elizabeth A.; MCKENNEY, Megan L.; MCNULTY, Oren T.; METCALF, Andrew T.; MORENO, David A.; RAMANN, Ginelle A.; TANG, Tony P.; REN, Li; WALLS, Shane M.; (946 pag.)WO2018/71454; (2018); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

138007-24-6, tert-Butyl piperidine-4-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(d) Ethyl 6-[4-(tert-butoxycarbonyl)piperidin-l-yl]-5-cyano-2-methylnicotinateA 20 mL microwave vial was charged with ethyl 6-chloro-5-cyano-2-methylnicotinate (5 g, 22.3 mmol), tert-butyl piperidine-4-carboxylate (4.11 g, 22.3 mmol), TEA (4.5 g, 44.5 mmol) and MeCN and heated, single nodeheating, to 100 0C for 5 minutes. The reaction was concentrated and MeCN/water was added to precipitate the product. Filtration of the solid and drying gave ethyl 6-[4-(tert-butoxycarbonyl)piperidin-l-yl]-5-cyano-2- methylnicotinate as an orange colored solid. Yield: 6.99 g (77percent). 1H NMR (400 MHz, DMSO-d6): delta 1.30 (3H, t), 1.40 (9H, s), 1.32-1.64 (2H, m), 1.88-1.96 (2H, m), 2.55-2.60 (IH, m), 2.63 (3H, s), 3.20-3-30 (2H, m), 4.24 (2H, q), 4.39-4.47 (2H, m), 8.31 (IH, s)., 138007-24-6

As the paragraph descriping shows that 138007-24-6 is playing an increasingly important role.

Reference£º
Patent; ASTRAZENECA AB; BYLUND, Ruth; HOVDAL, Daniel; JOHANSSON, Johan; SELLEN, Mikael; ZETTERBERG, Fredrik; WO2010/5385; (2010); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

88763-76-2, (R)-3-Aminopiperidin-2-one is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,88763-76-2

(R) -3-Aminopiperidine -2-one (1.00g, 8.76 mmol) in CH2Cl2 (15mL) triethylamine at room temperature to a solution (1.28mL, 9.2 mmol) and di-tert- butyl carbonate(2.01g, 9.2 mmol) It was added. The reaction mixture was stirred for 12 hours at the same temperature and concentrated under vacuum. The residual crude was diluted with ether (50 mL), and filtered through a pad of celite. The filtrate was evaporated to dryness, SiO2 chromatography (50g, EtOAc 100%) was purified by, 1.65g (88%) of 2-oxo-piperidin-3-yl carbamic acid (R) -tert- butyl colorless It was obtained as a foam.

The synthetic route of 88763-76-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; F.HOFFMANN-LA ROCHE AG; HENDRICKS, ROBERT THAN; HERMANN, JOHANNES CORNELIUS; KONDRU, RAMA K; LOU, YAN; LYNCH, STEPHEN M; OWENS, TIMOTHY D; SOTH, MICHAEL; (50 pag.)JP5667692; (2015); B2;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.2971-79-1,Methyl piperidine-4-carboxylate,as a common compound, the synthetic route is as follows.

EXAMPLE 6; 3-(l-(5-Ethylpyrimidin-2-yl)piperidin-4-yl)-N-(2-fluoro-4- (methylsulfonyl)phenyl)-[l,2,4]triazolo[4,3-a]pyrazin-8-amineStep 1. Methyl l-(5-ethylpyrimidin-2-yl)piperidine-4-carboxylate[0321] To a solution of methyl piperidine-4-carboxylate (7.1 g, 50 mmol) in DMF (50 mL), was added 2-chloro-5-ethylpyrimidine (14 g, 100 mmol) and diisopropylethylamine (10 mL). The reaction mixture was heated to 1000C for 2 h. The solution is then poured into ice water (500 mL), and extracted with ethyl acetate (2 x 200 mL). Purification by silica gel chromatography (gradient 10% to 50% ethyl acetate/hexanes) afforded methyl l-(5-ethylpyrimidin-2-yl)piperidine-4- carboxylate as a light yellow oil (8.6 g, 69%). LCMS: 250.2 (M+H)+., 2971-79-1

The synthetic route of 2971-79-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; KALYPSYS, INC.; KAHRAMAN, Mehmet; SMITH, Nicholas, D.; BONNEFOUS, Celine; NOBLE, Stewart, A.; PAYNE, Joseph, E.; WO2010/88518; (2010); 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.159874-38-1,Benzyl 4-(ethylamino)piperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

Method B; Preparation of ter/-butyl 4-{2-[ethyl(piperidin-4-yl)amino]-2-oxoethyl}piperazine-l- carboxylate.; Step 1: Preparation of tert-buty 4-{2-[{l-[(benzyloxy)carbonyl]piperidin-4-yl}(ethyl)amino]-2-oxoethyl}piperazine-l-carboxylate.; Diisopropylethylamine (1.3 ml) was added to a slurry of [4-(tert- butoxycarbonyl)piperazin-l-yl]acetic acid dihydrate (1.12g) [154478-71-6] in dichloromethane (16 ml) followed by HATU (1.82g) and the mixture was stirred under argon for 30 minutes. A solution of benzyl 4-(ethylarnino)piperidine-l-carboxylate (1.05g) [159874-38-1] in dichloromethane (4 ml) was added and the mixture was stirred for 24 hours, then diluted with dichloromethane (25 ml), washed consecutively with 2M NaOH (2×20 ml) and brine (1×20 ml) and dried. The solvent was evaporated and the residue was purified on a 4Og silica column eluted with a solvent gradient made up of ethyl acetate to 5% methanol: ethyl acetate. The yellow oil obtained was used directly in the next stage, LC-MS M+H 489 plus a HATU derived impurity M+H 175.1H NMR (CDCl3): 1.12 (3H, m), 1.44 (9H, s), 1.54-1.74 (8H, m), 2.48 (4H, d), 3.19-3.38 (4H, m), 3.44 (4H, d), 4.30 (IH, m), 5.14 (2H, s). 7.36 (5H, s)., 159874-38-1

159874-38-1 Benzyl 4-(ethylamino)piperidine-1-carboxylate 23369962, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2006/67385; (2006); 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.620611-27-0,tert-Butyl 4-(aminomethyl)-4-fluoropiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.,620611-27-0

[Reference Example 4] Synthesis of 4-fluoro-4-({[5-(methoxycarbonyl)benzimidazol-2-yl]amino}methyl)piperidinecarboxylic acid tert-butyl ester 4-(Aminomethyl)-4-fluoropiperidinecarboxylic acidtert-butyl ester (3.23 g, 13.9 mmol) was dissolved in acetonitrile (50 ml). A solution of thiocarbonyldiimidazole (2.73 g, 15.3 mmol) and triethylamine (4.27 ml, 30.6 mmol) in acetonitrile (20 ml) was then added dropwise at 0C of a period of 3 minutes. After stirring at room temperature for 1 hour, 3,4-diaminobenzoic acid methyl ester dihydrochloride (3.66 g, 15.3 mmol) was added to the reaction mixture, and the mixture was stirred at 50C for 5.5 hours. Diisopropylcarbodiimide (0.32 ml, 15.3 mmol) was further added and the mixture was stirred overnight at 50C. Saturated brine was added to the obtained reaction mixture, extraction was performed with ethyl acetate (200 ml), and the organic layer was dried overnight over anhydrous sodium sulfate. After filtration with a desiccant (anhydrous sodium sulfate) and concentration of the filtrate, the obtained brown oil was purified by silica gel column chromatography (CH2Cl2/MeOH = 49:1 ? 19:1) to obtain 4-fluoro-4-({[5-(methoxycarbonyl)benzimidazol-2-yl]amino}methyl)piperidinecarboxylic acid tert-butyl ester. The yield was 0.838 g (60%). 1H-NMR (270 MHz, CDCl3): delta1.43-1.95(m,5H), 1.45(s,9H), 3.06(brt,2H,J=11.3Hz), 3.50(s,3H), 3.67(d,2H,J=21.6Hz), 3.83-3.96(m,2H), 3.90(s,2H), 7.28(d,1H,J=8.4Hz), 7.81(dd,1H,J=1.6,8.4Hz), 7.90(brs,1H).

The synthetic route of 620611-27-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; TEIJIN LIMITED; EP1505067; (2005); 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.142752-12-3,1-(4-Aminophenyl)piperidin-4-ol,as a common compound, the synthetic route is as follows.

A mixture of starting material (12 mg, 0.05 mmol), 1-(4-aminophenyl)piperidin-4-ol (10 mg, 0.05 mmol), X-Phos (4.3 mg), Pd2(dba)3 (5.5 mg) and K2CO3 (30 mg, 0.22 mmol) in t-BuOH (1.0 mL) was heated at 85 C. in a seal tube for 4 h. The reaction was then filtered through celite, eluted with dichloromethane, and concentrated in vacuo. The residue was then purified by reverse-phase prep-HPLC to afford the title compound as the TFA salt (8.2 mg, 40%).

142752-12-3, As the paragraph descriping shows that 142752-12-3 is playing an increasingly important role.

Reference£º
Patent; DANA-FARBER CANCER INSTITUTE, INC.; Gray, Nathanael S.; Waller, David; Choi, Hwan Guen; Wang, Jinhua; Deng, Xianming; (104 pag.)US2016/24115; (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.1892-22-4,3-Aminopiperidin-2-one,as a common compound, the synthetic route is as follows.

To a solution of 0.1 g of 6-chloro-2-(3,5-dimethyl-1H-pyrazol-1-yl)-N-(3-(trifluoromethyl) phenyl) pyrimidin-4-amine [0735] in acetonitrile was added 3-amino-2-piperidone [0562] (0.062 g, 0.543 mmol) and N,N-diisopropyl ethylamine. The reaction mixture was heated at 180 C. under microwave for 5 h. The reaction mixture was concentrated under reduced pressure to afford crude product which was purified by column chromatography using 40% ethyl acetate in pet ether to afford 0.038 g of 3-((2-(3,5-dimethyl-1H-pyrazol-1-yl)-6-((3-(trifluoromethyl)phenyl)amino)pyrimidin-4-yl)amino) piperidin-2-one [0744], Compound 189 as a white solid. MS(M+1)+=446.2. 1H NMR (400 MHz, DMSO-d6) delta 9.52 (s, 1H), 8.55 (s, 1H), 7.69-7.66 (m, 2H), 7.47 (t, J=8.0 Hz, 2H), 7.23 (d, J=7.7 Hz, 1H), 6.05 (s, 1H), 5.82 (s, 1H), 4.43 (s, 1H), 3.17 (bs, 2H), 2.52 (s, 3H), 2.18 (s, 3H), 2.15-2.10 (m, 1H), 1.89-1.64 (m, 3H).

1892-22-4, The synthetic route of 1892-22-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Cadent Therapeutics, Inc.; Jefson, Martin R.; Keaney, Gregg F.; Larsen, Janus Schreiber; Lowe, III, John A.; McCall, John M.; (110 pag.)US2017/355708; (2017); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem