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CN100582092C 制备二苯基氮杂环丁烷酮衍生物的方法 失效 - 权利终止

制备二苯基氮杂环丁烷酮衍生物的方法
Abstract:
本发明涉及制备通式(I)的二苯基氮杂环丁烷酮衍生物或其取代基X、R1和/或R2被保护的形式的方法，见右式(Ⅰ)。其中的符号、取代基和标记具有下列含义：X＝H、OH；R1＝OH、OCH3；R2＝F、CH2CH3、CH2NHR4；R3＝H、F；R4＝H、CO-(CH2-)nCO-R5、CO-(CH2-)nNHR6；n＝4-16的整数；R5＝OH、NH-CH2-[CH(OH)-]mCH2OH；R6＝H、CO-[CH(OH)-]mCH2OH；m＝1-5的整数。根据所述方法，将通式(II)的新化合物，见右式(Ⅱ)。其中Y＝H，H；H，OH；H，OAc；H，OSi(烷基)o(芳基)p，o，p＝0、1、2或3且o+p＝3；H，OTHP；H，OC(芳基)3；H，OCH2O烷基；H，OCH(O烷基)CH3；H，O烷基；H，OCH2芳基；O烷基，O烷基；环状酮酰基如O-(CH2-)q-O，q＝2或3，与通式(III)的亚胺反应，见右式(Ⅲ)。其中R7＝R1以及O保护基且R8＝R2。
Abstract(English):

The invention relates to a method for producing diphenyl azetidinone derivatives of general formula (I) or forms protected in the substituents X, R<1> and/or R<2>, wherein the symbols, substituents, and indices have the following designations: X = H, OH; R = OH, OCH3; R<2> = F, CH2CH3, CH2NHR<4>; R<3> = H, F; R<4> = H, CO-(CH2-)nCO-R<5>, CO-(CH2-)nNHR<6>; n = whole numbers from 4 to 16; R<5> = OH, NH-CH2-[CH(OH)-]mCH2OH; R<6> = H, CO-[CH(OH)-]mCH2OH; and m = whole numbers from 1 to 5. According to said method, novel compounds of general formula (II), wherein Y = H, H; H, OH; H, OAc; H, OSi(alkyl)o(aryl)p where o, p = 0, 1, 2 or 3 and o + p = 3; H, OTHP; H, OC(Aryl)3; H, OCH2OAlkyl; H, OCH(OAlkyl)CH3; H, OAlkyl; H, OCH2aryl; Oalkyl, Oalkyl; and cyclic ketone acetyl such as O-(CH2-)q-O where q = 2 or 3, are reacted with imines of general formula (III) wherein R<7> = R<1> and O protective groups and R<8> = e.g. R<2>.

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