Category: 278788-60-6

278788-60-6, (R)-1-Boc-Piperazine-2-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Trimethylsilyl diazomethane (2M in hexane, 14 ml) was added dropwise to a solution of (2R)-L-(TERT-BUTOXYVARBONYL) piperazine-2-carboxylic acid (5 g) in methanol (100 ml) and DCM (115 ml), and the solution stirred at room temperature for 16 hours. The solvent was concentrated in vacuo and the residue purified by chromatography, eluting with ethyl acetate then 5% methanol / 7N ammonia in ethyl acetate, to give 1-tert-butyl 2-methyl (2R)- PIPERAZINE-1, 2-dicarboxylate as an oil (2.55 g, 48%); NMR spectrum (DMSO-d6) 1.40 (s, 9H), 2.10 (bs, 1H), 2.52 (m, 1H), 2.72 (dd, 1H), 2.82 (d, 1H), 2.97 (m, 1H), 3.29 (d, 1H), 3.61 (d, 1H), 3.67 (s, 3H), 4.43 (m, 1H) ; Mass spectrum MH+ 245.

278788-60-6, As the paragraph descriping shows that 278788-60-6 is playing an increasingly important role.

Reference：
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2005/26152; (2005); 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.278788-60-6,(R)-1-Boc-Piperazine-2-carboxylic acid,as a common compound, the synthetic route is as follows.

Trimethylsilyl diazomethane (2M in hexane, 14 ml) was added dropwise to a solution of (2R)-L-(TERT-BUTOXYVARBONYL) piperazine-2-carboxylic acid (5 g) in methanol (100 ml) and DCM (115 ml), and the solution stirred at room temperature for 16 hours. The solvent was concentrated in vacuo and the residue purified by chromatography, eluting with ethyl acetate then 5% methanol / 7N ammonia in ethyl acetate, to give 1-tert-butyl 2-methyl (2R)- PIPERAZINE-1, 2-dicarboxylate as an oil (2.55 g, 48%); NMR spectrum (DMSO-d6) 1.40 (s, 9H), 2.10 (bs, 1H), 2.52 (m, 1H), 2.72 (dd, 1H), 2.82 (d, 1H), 2.97 (m, 1H), 3.29 (d, 1H), 3.61 (d, 1H), 3.67 (s, 3H), 4.43 (m, 1H) ; Mass spectrum MH+ 245., 278788-60-6

278788-60-6 (R)-1-Boc-Piperazine-2-carboxylic acid 24820285, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2005/26152; (2005); 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.278788-60-6,(R)-1-Boc-Piperazine-2-carboxylic acid,as a common compound, the synthetic route is as follows.

(2R)-l-(ter^-Butoxycarbonyl)-4-ethylpiperazine-2-carboxylic acid; To (2i?)-l-(tert-butoxycarbonyl)piperazine-2-carboxylic acid (1.406 g) and Na2CO3 (2.59 g) was added dry EtOH (28 ml) then ethyl iodide (0.54 ml) and the mixture heated at reflux for 18 h under argon. The solvent was then removed under reduced pressure and 5percentMeOH/DCM (40 ml) was added and stirred for 1 hour in a sealed flask. The solution was filtered and washed with dichloromethane (2 x 1OmL). The filtrate was then placed directly onto a 120g-silica cartridge and was purified using eluent 10-70percent MeOH/DCM. After evaporation, the product was isolated as a white foam (1.00 g), which was used without further purification.

278788-60-6, The synthetic route of 278788-60-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2006/67401; (2006); 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.278788-60-6,(R)-1-Boc-Piperazine-2-carboxylic acid,as a common compound, the synthetic route is as follows.

PREPARATIVE EXAMPLE 6; The tricyclic alcohol [] (5.6 gm, 17.33 mmol) was dissolved in CH2Cl2 (56 mL) and SOCl2 (2.46 mL) was added while stirring under a dry N2 atmosphere. After 5 hrs. the tlc was checked ( by adding an aliquot of the reaction mixture to 1N NaOH and shaking with CH2Cl2 and checking the CH2Cl2 layer by tlc using 50percent EtOAc/Hexanes as the eluent). The mixture was evaporated to give a gum which was evporated from dry toluene twice and once from CH2Cl2 to give a foamy solid. The resulting chloro-tricyclic compound was dissolved in dry DMF (100 mL) and the title compound from Preparative Example 5 (3.98 gm) was added followed by triethylamine (12.11 mL) and the mixture stirred at ambient temperature under a nitrogen atmosphere. After 24 hours, the reaction mixture was concentrated and the residue dissolved in EtOAc (200 mL) and washed with brine. The brine layer was extracted with EtOAc (2X) and the combined organics were dried over MgSO4, filtered, and evaporated to give a foamy solid. The solid was chromatographed on a 1 1/2″ X 14″ column of silica gel eluting with 2L of 0.4percent 7N MeOH/NH3:CH2Cl2, 6L of 0.5percent 7N MeOH/NH3:CH2Cl2, 2L of 0.65percent 7N MeOH/NH3:CH2Cl2, 2L of 0..8percent 7N MeOH/NH3:CH2Cl2, 4L of 1percent 7N MeOH/NH3:CH2Cl2, 2L of 3percent 2N MeOH/NH3:CH2Cl2, 2L of 5percent 2N MeOH/NH3:CH2Cl2, 2L of 10percent 2N MeOH/NH3:CH2Cl2, 2L of 15percent 2N MeOH/NH3:CH2Cl2, 4L of 20percent 2N MeOH/NH3:CH2Cl2 to obtain 4.63 gm of final product.

278788-60-6, 278788-60-6 (R)-1-Boc-Piperazine-2-carboxylic acid 24820285, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; SCHERING CORPORATION; EP1140904; (2005); B1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics