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ChemicalBook CAS DataBase List N-Boc-Piperidine-4-carboxylic acid methyl ester

N-Boc-Piperidine-4-carboxylic acid methyl ester synthesis

12synthesis methods
2971-79-1 Synthesis
Methyl isonipecotate

2971-79-1
281 suppliers
$10.00/10g

24424-99-5 Synthesis
Di-tert-butyl dicarbonate

24424-99-5
821 suppliers
$13.50/25G

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Yield:124443-68-1 98%

Reaction Conditions:

with triethylamine in dichloromethane at 25; for 12 h;Product distribution / selectivity;

Steps:

A.2.1

Synthesis of 9-(Azetidin-1-yl)-9-phenyl-3-azaspiro[5.5]undecane Trifluoroacetate (A4); Step-1: 1-tert-Butyl 4-methyl piperidine-1,4-dicarboxylate; To a stirred solution of methyl isonipecotate (127.2 mmol, 1 eq) in dichloromethane (200 ml) were added di-tert-butyldicarbonate (190.8 mmol, 1.5 eq) and triethylamine (254.4 mmol, 2.0 eq). The reaction mixture was stirred for 12 h at 25° C. It was then diluted with dichloromethane (100 ml) and washed with water (50 ml) and brine (50 ml). The organic layer was separated, dried over Na2SO4, concentrated and employed in the next step without further purification. Yield: 98%

References:

US2010/113417,2010,A1 Location in patent:Page/Page column 36

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