VERFAHREN ZUR HERSTELLUNG VON KOMBINATORISCHEN AMINBIBLIOTHEKEN

    公开(公告)号:EP1087929A1

    公开(公告)日:2001-04-04

    申请号:EP99929282.4

    申请日:1999-06-18

    申请人: MERCK PATENT GmbH

    IPC分类号: C07C209/66 C07B61/00

    摘要: The invention relates to a method for producing a combinatory library comprising amines of general formula (I), whereby the method comprises a reaction of α components, said components being selected from compounds of general formula (II), whereby R?3, R4 and R5¿ represent the meanings cited in the description, with β components which are selected from compounds of general formulas (IIIa): Z-R?4 or Z-R5¿ or (IIIb): Z-R4-R5-Z, whereby R?4 and R5¿ have the meanings cited in the description and, in the instance of compounds of general formula (IIIb), the radicals R?4 and R5¿ are bound via a bonding; Z represents Li or MgX with X representing Hal and Hal representing Cl, Br, or I; α represents a whole number greater than or equal to 1, β represents a whole number greater than or equal to 1, whereby αβ2≥5. Said reaction is carried out in a solvent in the presence of a titanium, hafnium or zirconium compound and optionally in the presence of a co-catalyst.

    摘要翻译: 本发明涉及通式(I)的胺,其中R 1和R 2可以相同或不同,表示各自独立地取代或未取代的烷基,环烷基,烯基,环烯基,炔基, 芳基或三烷基甲硅烷基。 R 1和R 2也可以与它们所连接的氮原子一起形成取代或未取代的环烷基环,其可以与氮原子一起含有至少一个选自以下的基团的其它杂原子: 氮,氧和硫。 R 3选自氢和可以被1至3个氟原子取代的甲基,而R 4和R 5可以相同或不同,并且各自独立地表示烷基,环烷基,烯基,环烯基, 炔基或取代或未取代的芳基。 R 4和R 5也可以表示被取代或未取代的芳基,环烷基,烯基,环烯基或炔基取代的烷基,条件是至少一个R 4和R 5基团 包括芳基。 本发明还涉及其盐。