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    • 96. 发明申请
    • NEW PROCESS FOR MANUFACTURING OPTICALLY ACTIVE CARBOCYCLINE INTERMEDIATES
    • 制造光学活性炭中间体的新工艺
    • WO1988003526A1
    • 1988-05-19
    • PCT/DE1987000515
    • 1987-11-12
    • SCHERING AKTIENGESELLSCHAFTSKUBALLA, WernerDAHL, Helmut
    • SCHERING AKTIENGESELLSCHAFT
    • C07C177/00
    • C07D319/08C07C405/0083
    • Process for manufacturing cis-bicyclo[3.3.0]octane-2-aldehydes of formula (I), in which R1 and R2 jointly represent the double-bound residue -O-X-O-, with X as straight or branched-chain alkylene with 1-7 C-atoms or R1 and R2 accordingly represent the residue OR with R as a straight or branched-chain alkyl with 1-7 C atoms and R3 represents hydrogen, a saturated alkyl residue with 1-7 C atoms, an aralkyl residu with 7-10 C atoms, a tetrahydropyranyl residue, a trialkylsilyl residue with 1-6 C atoms in the alkyl whereby alkyl also can be substituted by phenyl, a dialkylphenylsilyl residue or alkyldiphenylsilyl residue with 1-16 C atoms in the alkyl, characterized by the fact that the diastereomeric amides of formula (II) are separated, whereby in said formula R1, R2 and R3 have the stated meanings, and in that the enantiomerically pure amide of formula (II) is reduced.
    • 制备式(I)的顺式 - 双环[3.3.0]辛烷-2-醛的方法,其中R 1和R 2共同代表双键残基-OXO-,X为直链或支链亚烷基, 7个C原子或R 1和R 2相应地表示残基OR,其中R为具有1-7个C原子的直链或支链烷基,R 3表示氢,具有1-7个C原子的饱和烷基残基,残基为7 -10 C原子,四氢吡喃基残基,烷基中含有1-6个C原子的三烷基甲硅烷基残基,其中烷基也可以被苯基,二烷基苯基甲硅烷基残基或烷基中具有1-16个碳原子的烷基二苯基甲硅烷基残基取代,其特征在于 分离式(II)的非对映体酰胺,其中在所述式R1中,R2和R3具有所述含义,并且由式(II)的对映体纯的酰胺还原。
    • 98. 发明申请
    • CARBACYCLINE, PREPARATION AND UTILIZATION THEREOF
    • 卡巴肼,其制备和利用
    • WO1983003248A1
    • 1983-09-29
    • PCT/DE1983000045
    • 1983-03-11
    • SCHERING AKTIENGESELLSCHAFTVORBRÜGGEN, HelmutRADÜCHEL, BerndSKUBALLA, WernerSCHWARZ, NorbertCASALS-STENZEL, JorgeMANNESMANN, GerdaTOWN, Michael-Harold
    • SCHERING AKTIENGESELLSCHAFT
    • C07C177/00
    • C07D317/72C07C45/59C07C57/26C07C57/60C07C405/0083C07D263/14C07F9/4018C07C49/743
    • Carbacycline derivatives having the formula I wherein R1 is the residue CH2OH or -C-OR2, R2 representing a hydrogen atom, an alkyl, cycloalkyl, aryl, CH2 -C-aryl residue or a heterocyclic residue, or R1 is the residue -C-NHR3, R3 representing an alkanoyl or alkanesulfonyl residue containing each 1 to 10 atoms of carbon or the residue R2 or R1 is the residue wherein m is 1 or 2. X is an oxygen atom or CH2 group, A is a trans -CH=CH- or -C=C- group, W is a free or modified hydrocymethylene group wherein the OH group may be in the position alpha or beta , n represents the integer 1, 2 or 3, D is a straight chain alkylene group with 1 to 3 atoms of carbon, E represents a -C=C- bond or a -CR6=CR7 group, R6 and R7 being different and representing a hydrogen atom or an alkyl group with 1 to 5 atoms of carbon or a hydrogen atom or an a halogen atom, preferably chlorine, R4 represents an alkyl, cycloalkyl group or an optionally substituted aryl group or a heterocyclic group, R5 represents a free or modified hydroxy group. When R2 represents a hydrogen atom, the salts of compounds with pharmaceutically acceptable bases are also involved. The compounds are used as hypotensive agents.
    • 具有式I的卡巴环素衍生物,其中R 1是残基CH 2 OH或-CON OR 2,R 2表示氢原子,烷基,环烷基,芳基,CH 2 -C芳基或杂环残基,或R 1 是残基,如表示含有1-10个碳原子的链烷酰基或烷磺酰基残基,R 2或R 1为残基,其中m为1或2.X为氧原子 或CH 2基团,A是反式-CH = CH-或-C = C-基团,W是游离或修饰的水合甲基基团,其中OH基团可以在α或β位置,n表示整数1,2或 3,D是具有1至3个碳原子的直链亚烷基,E表示-C = C-键或-CR 6 = CR 7基团,R 6和R 7不同,表示氢原子或具有1个 至5原子的碳或氢原子或卤素原子,优选氯,R4表示烷基,环烷基或任选取代的芳基或杂环 酰基,R5表示游离或改性的羟基。 当R 2表示氢原子时,也涉及具有药学上可接受的碱的化合物的盐。 这些化合物用作降压剂。
    • 99. 发明申请
    • BISSTEROIDAL COMPOUNDS AND THEIR USE FOR THE PREPARATION OF CHIRAL COMPLEXES
    • 双组分化合物及其用于制备复合物的用途
    • WO1998028322A1
    • 1998-07-02
    • PCT/EP1997007098
    • 1997-12-18
    • SCHERING AKTIENGESELLSCHAFTMOHR, Jörg-TorstenENEV, ValentienEWERS, ChristianHARRE, MichaelHICKISCH, Klaus
    • SCHERING AKTIENGESELLSCHAFT
    • C07J01/00
    • C07J31/006C07J1/0055C07J1/0077C07J51/00
    • Bissteroidal compounds of general formula (I), in which R1 stands for hydrogen, alkyl, acyl, fluorine, and X1R5, where X1 stands for oxygen and sulfur and R5 can either be hydrogen, alkyl, aryl; R2 stands for hydrogen and alkyl; the stereochemistry of C-13, C-14 and C-17 may either be a or b; X stands for oxygen, hydroxyl, trifluormethylsulfonyloxy, or (R6)2P, where R6 can be aryl, alkyl and cycloalkyl; R3 stands for hydrogen, alkyl, aryl, trialkylsilyl, fluorine and X2R6, where X2 stands for oxygen and sulfur and R6 stands for hydrogen, trifluormethylsulfonyl, alkyl, cycloalkyl or aryl. R4 can either be a substituent in the 6 or 7 position of the steroid with the meaning of hydrogen, alkyl, aryl, fluorine, and X3R7, where X3 stands for oxygen, sulfur or trialkylsilyl and R7 stands for hydrogen, trifluormethylsulfonyl, alkyl or aryl, and the B-ring of the steroid contains none or two double bonds. Enantio- and Diastereomeric derivatives of compounds of general formula (I), metal complexes thereof and their use in enantioselective reactions.
    • 通式(I)的双星型化合物,其中R1代表氢,烷基,酰基,氟和X1R5,其中X1代表氧和硫,R5可以是氢,烷基,芳基; R2代表氢和烷基; C-13,C-14和C-17的立体化学可能是a或b; X代表氧,羟基,三氟甲基磺酰氧基或(R6)2P,其中R6可以是芳基,烷基和环烷基; R3代表氢,烷基,芳基,三烷基甲硅烷基,氟和X2R6,其中X2代表氧和硫,R6代表氢,三氟甲基磺酰基,烷基,环烷基或芳基。 R4可以是类固醇6或7位的取代基,具有氢,烷基,芳基,氟和X3R7的含义,其中X3表示氧,硫或三烷基甲硅烷基,R7表示氢,三氟甲磺酰基,烷基或芳基 ,并且类固醇的B环含有无或两个双键。 通式(I)化合物的对映异构体和非对映体衍生物,其金属络合物及其在对映选择性反应中的用途。