PROBLEM TO BE SOLVED: To provide a method for efficiently producing at low cost, high-purity chiral 8-(3-amino-piperidin-1-yl)-xanthine as an enantiomer by using a chemically, optically highly-pure starting material.SOLUTION: There is provided a method for preparation of a compound of formula (I) (wherein R1 is quinazolinylmethyl R2 is methyl and R3 is 2-butyn-1-yl), an enantiomer or salt thereof, comprising reacting a xanthine derivative having a halogen atom or the like at the eighth position and 3-phthalimidopiperidine being raw materials and then performing a deprotection reaction.COPYRIGHT: (C)2013,JPO&INPIT【課題】低コストで効率よく、化学的かつ光学的に高純度の出発物質を使用して、鏡像体として高純度のキラル8-(3-アミノピペリジン-1-イル)-キサンチンを製造する方法の提供。【解決手段】原料化合物である、8位にハロゲン原子等を有するキサンチン誘導体と3-(フタルイミド)ピペリジンを反応させ、次に脱保護反応を行う、式(I)の化合物、その鏡像体もしくは塩の調製方法。(式中、R1はキナゾリニルメチル基、R2はメチル基、R3は2-ブチン-1-イル基である)【選択図】なし
