Simple exploration of 78818-15-2

The synthetic route of 78818-15-2 has been constantly updated, and we look forward to future research findings.

78818-15-2, Benzyl 3-oxopiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,78818-15-2

EXAMPLE A; Preparation of Compound A of Formula 1 Process for the Preparation of Compound A-In-2:[00118] This compound was prepared by the method described by Bryant, HJ. et al, in WO 01/44250.[00119] To a stirred and cold (ice-bath cooling) suspension of benzyl 3- oxopiperazine-1-carboxylate (A-In-I) (1.00 g) and K2CO3 (11.8 g) in CH2Cl2 (40 mL) was added under N2 trimethyloxonium tetrafluoroborate (2.20 g, from Aldrich) in one portion. The cooling bath was removed and the mixture was stirred at room temperature under N2 for 19 h. This mixture was poured into water (40 mL) under ice-cooling and the organic phase was collected. The aqueous phase was extracted with CH2Cl2. The combined CH2Cl2 phases were washed with water (20 mL), then with brine, dried (Na2SO4) and concentrated. The crude residual oil was purified by silica gel column chromatography (5% MeOH/CH2Cl2) to give the title compound A- In-2 as colorless oil.

The synthetic route of 78818-15-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BRISTOL-MYERS SQUIBB COMPANY; WO2009/158394; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Some tips on 78818-15-2

The synthetic route of 78818-15-2 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.78818-15-2,Benzyl 3-oxopiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

78818-15-2, EXAMPLE 89 1-(4-Chloroquinolin-7-ylmethyl)-piperazin-2-one. 4-(Benzyloxycarbonyl)-piperazin-2-one (1.1 g, 4.6 mmol) is dissolved in THF (50 ML), cooled in an ice bath and treated with tretrabutylammonium iodide (0.18 g, mmol) and 60% sodium hydride (0.24 g, 6.0 mmol).The reaction mixture is stirred at 0 C. for 30 minutes then treated dropwise with a solution of 7-bromomethyl-4-chloroquinoline (1.2 g, 4.6 mmol), Example 14, in THF (50 ML).The resulting solution is stirred at 0 C. for 2 h then quenched with ammonium chloride solution and concentrated.Dilution with ethyl acetate is followed by a water wash; the organic layer is dried (sodium sulfate) and concentrated.The residue is chromatographed (4% methanol/methylene chloride) to yield solid 4-(benzyloxycarbonyl)-1-(4-chloroquinolin-7-ylmethyl)-piperazin-2-one (1.2 g, 2.9 mmol).A portion of this material (0.75 g, 1.8 mmol) is dissolved in acetonitrile (20 ML) and treated with iodo trimethylsilane (0.78 ML, 5.4 mmol) at room temperature for 3 hours.The reaction is quenched with methanol and concentrated to dryness.methanol addition and concentration is repeated four times.The final residue is taken up is 2M aqueous HCl; the solution is washed with ether and concentrated.The residue is recrystallized from isopropanol and ether to yield the title compound (0.63 g, 2.3 mmol) MS m/z: M+=275; 1HNMR (CD3OD, 300 MHz) delta9.1 (d, 1H), 8.5 (d, 1H), 8.2-8.3 (m, 2H), 8.0 (d, 1H), 5.2 (s, 2H), 4.1 (s, 2H), 3.7-3.8 (m, 2H), 3.6-3.7 (m, 2H).

The synthetic route of 78818-15-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; AVENTIS PHARMACEUTICALS INC.; US2004/102450; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Brief introduction of 78818-15-2

As the paragraph descriping shows that 78818-15-2 is playing an increasingly important role.

78818-15-2, Benzyl 3-oxopiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

78818-15-2, [0921] To the solution of XXIV-1 (20 g, 85.5 mmol) in DMF (100 mL) was added NaH (60%, 4.1 g, 103 mmol) in portions. The mixture was stirred at rt for 30 min. Then XXIV-2 (14.3 g, 85.5 mmol) was added. The reaction was stirred at rt overnight. The reaction was quenched with ice-water carefully, and then extracted with EtOAc (100 mL¡Á2). The combined organic layer was washed with brine, dried over anhydrous Na2SO4 and concentrated. The residue was used for next step directly (40 g, 140% crude yield).

As the paragraph descriping shows that 78818-15-2 is playing an increasingly important role.

Reference£º
Patent; Buckman, Brad Owen; Nicholas, John Beamond; Ramphal, Johnnie Y.; Emayan, Kumaraswamy; Seiwert, Scott D.; US2014/94456; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Some tips on 78818-15-2

The synthetic route of 78818-15-2 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.78818-15-2,Benzyl 3-oxopiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.,78818-15-2

Step A: 5-Ethoxy-3,6-dihydro-2H-pyrazine-1-carboxylic acid benzyl ester To a solution of 3-oxo-piperazine-1-carboxylic acid benzyl ester (2.0 g, 8.54 mmol, Maybridge) in dichloromethane (18 mL) at room temperature was added triethyloxonium tetrafluoroborate (4.1 g, 21.3 mmol). This mixture was allowed to stir for about 3 days then quenched by the addition of ice chips followed by saturated aqueous sodium bicarbonate until a neutral pH was obtained. The organic layer was separated and the aqueous layer was extracted with chloroform (3*). The combined organic extracts were washed with brine (1*), dried over sodium sulfate, and concentrated to give 2.11 g (95%) of the title compound of Example 259, Step A as a slightly yellow oil that was sufficiently pure to carry on to the next step. 1H NMR (CDCl3, 300 MHz) delta7.43-6.97 (c, 5H), 5.17 (s, 2H), 4.10 (q, 2H), 3.98 (s, 2H), 3.60-3.40 (c, 4H), 1.27 (t, 3H); MS (APCI) 263 (MH+).

The synthetic route of 78818-15-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Pfizer Inc.; US6414149; (2002); B1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics