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Production of 3-beta-aminonortropane derivatives, useful as e.g. N-methyl-D-aspartate receptor modulators, or synthetic intermediates, comprises preparing an imine, converting the imine into a stable tautomer or isomer, and hydrolyzing
Production of 3-beta-aminonortropane derivatives, useful as e.g. N-methyl-D-aspartate receptor modulators, or synthetic intermediates, comprises preparing an imine, converting the imine into a stable tautomer or isomer, and hydrolyzing
Producing 3-beta -aminonortropane derivatives (I) comprises preparing an imine (IVA) or (IVB) by reacting a 3-tropanone derivative (IIA) with an arylmethylamine or reacting a 3-alpha -aminonortropane derivative (IIB) with an araldehyde, converting the imine into a thermodynamically stable tautomer or isomer (V), and hydrolyzing (V). Producing 3-beta -aminonortropane derivatives of formula (I) comprises preparing an imine of formula (IVA) or (IVB) by reacting a 3-tropanone derivative of formula (IIA) with an arylmethylamine ArCH 2NH 2 or reacting a 3-alpha -aminonortropane derivative of formula (IIB) with an araldehyde ArCHO, converting the imine into a thermodynamically stable tautomer or isomer of formula (V), and hydrolyzing (V). [Image] R 11-8C alkyl, 2-8C alkenyl, 3-8C cycloalkyl or (6-10C)aryl(1-8C)alkyl; Ar : optionally substituted phenyl or 5- or 6-membered heteroaryl. An independent claim is also included for imines of formula (IVA), (IVB) and (V). ACTIVITY : None given. MECHANISM OF ACTION : N-methyl-D-aspartate receptor modulator.
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机译：制备3-β-氨基降冰片烷衍生物（I）包括通过使3-泛酮衍生物（IIA）与芳基甲胺反应或使3-α-氨基降冰片烷衍生物（IIB）与芳醛反应来制备亚胺（IVA）或（IVB），将亚胺转化为热力学稳定的互变异构体或异构体（V），然后水解（V）。制备式（I）的3-β-氨基降冰片烷衍生物包括通过使式（IIA）的3- 3-酮衍生物与芳基甲胺ArCH 2NH 2反应或使3-α-具有芳醛ArCHO的式（IIB）的氨基降冰片烷衍生物，将亚胺转化成热力学稳定的式（V）的互变异构体或异构体，并水解（V）。 [图像] R 1> 1-8C烷基，2-8C烯基，3-8C环烷基或（6-10C）芳基（1-8C）烷基; Ar：任选取代的苯基或5-或6-元杂芳基。对于式（IVA），（IVB）和（V）的亚胺也包括独立权利要求。活动：未提供。作用机理：N-甲基-D-天冬氨酸受体调节剂。
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