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    12.
    发明专利
    未知

    公开(公告)号：DK131905C

    公开(公告)日：1976-02-23

    申请号：DK587767

    申请日：1967-11-23

    Applicant: HOECHST AG

    Inventor： HOECHST AG

    IPC: C07D265/18

    Abstract: 2-Amino-4,4-di-substituted benzoxazine derivatives and the salts thereof with a physiologically compatible acid have an action on the central nervous system. These benzoxazines have the formula IN WHICH R is hydrogen, alkyl of one to four carbon atoms, cyclohexyl, phenyl or benzyl, R1 is hydrogen, halogen, trifluoromethyl, R2 is alkyl of one to four carbon atoms and R3 is phenyl or halophenyl.

    13.
    发明专利
    未知

    公开(公告)号：DK131905B

    公开(公告)日：1975-09-22

    申请号：DK587767

    申请日：1967-11-23

    Applicant: HOECHST AG

    Inventor： HOECHST AG

    IPC: C07D265/18

    Abstract: 2-Amino-4,4-di-substituted benzoxazine derivatives and the salts thereof with a physiologically compatible acid have an action on the central nervous system. These benzoxazines have the formula IN WHICH R is hydrogen, alkyl of one to four carbon atoms, cyclohexyl, phenyl or benzyl, R1 is hydrogen, halogen, trifluoromethyl, R2 is alkyl of one to four carbon atoms and R3 is phenyl or halophenyl.

    14.
    发明专利
    未知

    公开(公告)号：DK131903B

    公开(公告)日：1975-09-22

    申请号：DK349765

    申请日：1965-07-08

    Applicant: HOECHST AG

    Inventor： HOECHST AG

    IPC: A61K31/195 ,  C07C101/08

    Abstract: L - (-) - b - (3,4 - Dihydroxyphenyl) - a - methylalanine (" L-a -methyl-DOPA ") is made by splitting a benzyl methyl malonic monoester of the Formula II in which R is CH3 and R1 is CH3, C4H9n or benzyl and, if R1 is CH3, R may also be a benzyl or allyl radical, into its antipodes by means of an optically active base and then (A) converting the D compound of Formula II obtained into an optically inactive symmetrical di-ester by esterification with an alcohol R1OH and then converting into the inactive starting material of Formula II by hydrolysing one ester group, and (B) converting the L-compound of Formula II into the desired L-a -methyl-DOPA by (a) converting into an L-isocyanate (in which R1 is the same as R but cannot be allyl) and thence into an amino compound wherein R2 is a hydrogen atom or an acyl or carbalkoxy radical and splitting off the etherifying radicals R1, the esterifying radical R1 and any N-acyl or N-carbalkoxy group by hydrolysis or, in the case when R1 is benzyl, by hydrogenation and hydrolysis; or (b) when R is an allyl radical, hydrogenating to convert the allyl groups to n-propyl groups, converting the product by known methods, e.g. via the azide, isocyanate and carbamic ester, into an amine of the formula in which R3 is hydrogen or CH3 and splitting off the propyl groups, together with the methyl group R3 if present and any N-acyl or N-carbalkoxy group present, by the action of strong hydrohalic acids; or (c) when R is an allyl radical, converting into the amino compound and treating this by (i) reacting with a hydrohalic acid, or (ii) hydrogenating and reacting with a strong hydrohalic acid, or (iii) splitting off one allyl group together with any esterifying methyl group or N-acyl or N-carbalkoxy group by reaction with an alkali-metal alkoxide and either treating with a hydrohalic acid or hydrogenating and treating with a hydrohalic acid to remove the second allyl group. Symmetrical di-esters of the formula used for the preparation of the mono-ester starting material II are made by condensing a malonic di-ester of the formula CH2(COOR1)2 with 3,4-dihydroxybenzaldehyde or its methyl ethers and hydrogenating and C-methylating the resulting 3,4-dihydroxybenzylidene malonic acid di-ester or corresponding methylated compound. The corresponding 3,4-di-allyl or 3,4-dibenzyl ethers are obtained by allylation or benzylation of the 3,4-dihydroxy benzylmalonic di-esters and the products may, if desired, be re-esterified thus, for example, converting a di-methyl ester into a di-benzyl or di-n-butyl ester.

    18.
    发明专利
    未知

    公开(公告)号：BR6680180D0

    公开(公告)日：1973-12-26

    申请号：BR18018066

    申请日：1966-06-03

    Applicant: HOECHST AG

    Inventor： HOECHST AG

    IPC: B02C18/06 ,  C07D219/02 ,  C07D219/04 ,  C07D219/06 ,  C07D219/14 ,  C07D265/18 ,  C07D265/38

    Abstract: (A) 3,1-Benzothiazines and 3,1-benzoxazines of gen. formula (I), where A = O or S R = H, alkyl, cycloalkyl, alkenyl, cycloalkenyl aryl, aralkyl, or lower dialkylaminoalkyl in which the dialkylamino group can also be cyclized via O, S, or methyl- or benzylimino, R1 = H, halogen, methoxy, CF3, NO2 R2 = alkyl, aralkyl, or aryl, in which the benzene rings of the last two can be substituted by halogen, methoxy, CF3, NO2. (B) Salts of I formed with organic and inorganic acids. Compounds (1) combine valuable pharmacological properties with very low toxicity. They are central depressants, as well as stimulants, sedatives, noradrenaline potentiators, analgesics and spasmolytics, and they prolong narcosis. They are useful in the treatment of mental diseases, e.g. depression, psychioneuroses, disturbances and anxiety states of neurotic and psychotic patients.

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