Abstract: A new process for the production of .beta.-carbolines by dehydrogenation of tetrahydro-.beta.-carbolines with trichloroisocyanuric acid is described.

Abstract: A process for the production of indole derivatives, which is characterized in that in the presence of phosphoric acid a substitution with an imine is performed, and intermediate products of this process and the production of these intermediate products are described.

Abstract: A process for the production of ergoline derivatives of general formula I is described ##STR1## in which the bonds represent two single-bonds or a double bond and a single bond.R.sub.1 means a hydrogen atom or an alkyl group with 1-6 carbon atomsR.sub.2 symbolizes a hydrogen atom or an alkyl group with 1-6 carbon atoms,R.sub.3 represents a carboxyl group or a grouping of formula--CONR.sub.4 R.sub.5 or --NHCQNR.sub.6 R.sub.7with R.sub.4 and R.sub.5 meaning hydrogen or an alkyl radical with 1-6 carbons atoms optionally substituted by a hydroxy group and R.sub.6 and R.sub.7 meaning an alkyl group containing 1-4 carbon atoms and Q meaning an oxygen or sulfur atom.

Abstract: Disclosed is chemoselective phenylation of 5-hydroxy-.beta.-carbolines in the presence of weak bases while adding water.

Abstract: A process for the production of gramine derivatives is described, which is characterized in that an indole is reacted with an imine under acid catalysis in the presence of primary amines.

Abstract: 2-bromo-8-ergolinyl compounds of the formula ##STR1## wherein R.sup.8 is NH.sub.2, NH--CONEt.sub.2, CONH.sub.2, ##STR2## and ##STR3## wherein R.sup.1 =C.sub.1-4 -alkyl andR.sup.2 =C.sub.1-4 -alkyl and benzyl,R.sup.9 and R.sup.10 each mean hydrogen or, together, a bond, and the substituent R.sup.8 can be in the .alpha.- or .beta.- position, and their acid addition salts,can be prepared from corresponding 8-ergolinyl compounds and their acid addition salts by bromination with elemental bromine in the presence of hydrogen bromide in a halogenated hydrocarbon.

Abstract: Ergoline derivatives of general Formula I ##STR1## wherein C.sub.8 C.sub.9 and C.sub.9 C.sub.10 are both CC-single bonds or one is a C.dbd.C-double bond,R.sup.6 is C.sub.1-4 alkyl,R.sup.8 is methyl, hydroxymethyl, carbonylmethoxy, ureido or N,N-diethylureido, each in the .alpha.- or .beta.-position, andR is hydrogen or nitro,are prepared by dehydrogenation of corresponding 2,3-dihydroergoline derivatives using an electrophilic reagent in an apolar solvent and a base.

Abstract: Ergolinyl compounds which are nitrogen-substituted in the 8-position and have Formula (I) ##STR1## and physiologically compatible salts thereof, wherein (a) R.sup.1 is hydrogen, the 8-substituent can be in the .alpha.- or .beta.-position and ##STR2## represents a single or a double bond, R.sup.2 is hydrogen, C.sub.1-4 -alkyl or C.sub.1-7 -acyl,R.sup.3 is hydrogen, chlorine or bromine, andR.sup.4 is C.sub.1-6 -alkyl, C.sub.3-6 -cycloalkyl-C.sub.1-3 -alkyl, C.sub.3-6 -alkenyl, or C.sub.3-6 -alkynyl; or(b) R.sup.1 is ##STR3## and the 8-substituent can be in the .alpha.- or .beta.-position, ##STR4## represents a single or double bond, R.sup.2, R.sup.3 are as defined above,R.sup.4, is C.sub.1.varies.6 -alkyl, C.sub.3-6 -cycloalkyl-C.sub.1-3 -alkyl, C.sub.3-6 -alkenyl, or C.sub.3-6 -alkynyl; andR.sup.5 is hydrogen, C.sub.-10 -alkyl, C.sub.3-10 -alkenyl, or C.sub.3-10 -alkynyl, andR.sup.6 is C.sub.1-10 -alkyl, C.sub.3-10 -alkenyl, C.sub.3-10 -alkynyl, or aryl, orR.sup.5 and R.sup.

Abstract: Ergolinylthioureas derivatives of the general Formula I ##STR1## wherein R.sup.1 is hydrogen, lower alkyl or acyl,R.sup.2 is hydrogen, halogen or a lower alkylthio groupR.sup.3 is lower alkyl,R.sup.4, R.sup.5 and R.sup.6, is hydrogen or lower alkyl, and each is identical or different,n=0, 1 or 2 and C.sub.9 --C.sub.10 is a single or a double bond; are produced by reacting in an ergolin-8-ylurea compound otherwise corresponding to Formula I with a --CO--NR.sup.5 R.sup.6 group in place of the --CS--Nr.sup.5 R.sup.6 group is reacted with a chlorinating agent and a thiolating agent.

Abstract: Substituted ergolines of the formula ##STR1## and their acid addition salts, wherein the urea side chain in the 8-position can be in the d.alpha.- or .beta.-configuration, C.sub.2 C.sub.3 and C.sub.9 C.sub.10 are a CC single or C.dbd.C double bond, andR is hydrogen or NR'R" wherein R'R" is O.sub.2, H.sub.2, C.sub.1-4 -dialkyl, or, together, they form a 3- to 9-membered ring, or R' and R" individually are hydrogen, C.sub.1-4 -alkyl, or C.sub.1-10- -acyl,R.sup.1 is hydrogen, C.sub.1-4 -alkyl, C.sub.1-10 -acyl, C.sub.6-8 -aryl, or C.sub.1-4 -alkylsulfonyl,R.sup.2 is hydrogen or halogen if C.sub.2 C.sub.3 is a C.dbd.C double bond, or hydrogen if C.sub.2 C.sub.3 is a CC single bond,R.sup.6 is C.sub.1-4 -alkyl,show a pronounced effect on the central nervous system and are suitable, for example, as antidepressants, neuroleptics, or antihypertensives.

Abstract: A process for preparing an ergoline of the formula ##STR1## wherein C.sub.9 ----C.sub.10 is a CC single or double bond,R.sup.1 is hydrogen or CONR.sub.2, R being hydrogen, methyl, or ethyl, and wherein NR' is in the .alpha.- or .beta.- position,R.sup.2 is lower alkyl of up to 3 carbon atoms, and the salts thereof,comprises treating the corresponding ergolinyl carboxylic acid amide with lead(IV) acetate in an aprotic polar solvent; reacting the intermediarily formed corresponding isocyanate with water or with a reactive amine of up to 4 carbon atoms, (e.g. a mono- or dialkylamine of up to 4-C atoms); and, optionally, treating the resultant product with an acid to form the corresponding salt.

Abstract: 2-bromoergolines can be reduced in good yields, without dimerization as determined by NMR product analysis, to the corresponding 2,3-dihydroergolines under otherwise conventional reducing conditions by introducing 2-bromoergolines, together with sodium borohydride, into trifluoroacetic acid under cooling to prevent the reaction mixture from rising above ambient temperature.

Abstract: .beta.-carbolines of formula I ##STR1## wherein R=C.sub.1-5 alkylR.sup.4 =H, C.sub.1-5 alkyl or --(CH.sub.2).sub.n --OR with n=1 or 2 andR.sup.A =H, R, (CHR).sub.n --OR, OCH.sub.2 Ph, OPh, OPh(Cl,Br),OR,OCH.sub.2 Ph(Cl,Br) NRR, Cl or Br,wherein n and R have the above meanings and there are one or two R.sup.A 's are prepared, by dehydrogenation at reaction temperatures below ambient temperature in an inert solvent with tert-butyl hypochlorite and a tertiary amine.

Abstract: A process for preparing lysergic acid esters of the formula ##STR1## wherein R is alkyl of up to 3 carbon atoms, comprises reacting corresponding lysergic acid or isolysergic acid amides with corresponding alcohols at temperatures of 0.degree. to 65.degree. C. for 2 to 30 hours in the presence of an acid at a pH value of 0-1.

Abstract: 16 .alpha.-Alkyl steroids of the formula ##STR1## wherein R.sub.1 is hydrogen or methyl,R.sub.2 is hydrogen, alkyl, acyl, or glycosylR.sub.3 is hydrogen or a substituted or unsubstituted, saturated or unsaturated lower hydrocarbon residue, andR.sub.4 is methyl, ethyl or propyl, exhibit strong progestational activity and a very low androgenic activity.

Abstract: 16-dimethylaminomethylene-3-methoxy-1,3,5(10)-estratrien-17-one is a valuable new preparative intermediate which may be used, e.g., to prepare 17.beta.-hydroxy-16.beta.-ethyl-4-estren-3-one or 16.beta.-ethylestradiol.

Abstract: Bicycloalkane derivatives of the formula ##STR1## wherein n is 1 or 2, R.sub.1 is lower alkyl, Acyl is alkanoyl, and Y is --S--R.sub.2, --SO.sub.m --R.sub.2, or ##STR2## wherein m is 1 or 2, R.sub.2 is alkyl, R.sub.3 is hydrogen or lower alkyl, R.sub.4 is acyl or phenyl optionally substituted with lower alkoxy, benzyloxy or alkanoyloxy; and Z is nitro, lower alkoxycarbonyl, lower alkanoyl, lower alkylsulfinyl, or lower alkylsulfonyl are useful intermediates in the total synthesis of steroids. The compounds are prepared by reacting a corresponding compound lacking the CH.sub.2 Y substituent with formaldehyde and a mercaptan or sulfinic acid, followed if desired by oxidation and optional salt condensation.

Abstract: C-homoestratrienes of the formula ##STR1## wherein ##STR2## R.sub.1 and R.sub.2 are the same or different, and each is hydrogen, acyl, alkyl, cycloalkyl or tetrahydropyranyl; andR.sub.3 is hydrogen, ethynyl or chloroethynyl; possess very good estrogenic properties.

Abstract: Sterol derivatives of the formula ##STR1## wherein R.sub.1 is a hydrogen atom and R.sub.2 is lower alkoxy, or R.sub.1 and R.sub.2 collectively are lower alkylenedioxy and R.sub.3 is a sterol hydrocarbon side chain are converted to the corresponding androsten-17-ones by the oxidative degradation activity of a species of microorganism which degrades sterol side chains, preferably of the genus Mycobacterium. The ether group of those compounds wherein R.sub.1 is a hydrogen atom and R.sub.2 is lower alkoxy, and the corresponding 17.beta.-hydroxy and 17.alpha.-hydrocarbon-17.beta.-hydroxy compounds is cleaved by reaction with an alkanoic acid chloride or anhydride in the presence of a Lewis acid.

Abstract: A process for the preparation of 17.beta.-hydroxy-20-alkoxypregnane-21-oic acid derivatives of the formula ##STR1## WHEREIN R.sub.1 is methyl or ethyl;R.sub.2 is hydrogen or methyl, either being in the .alpha.-or .beta.-position;R.sub.3 is lower alkyl of 1-4 carbon atoms;R.sub.4 is alkyl of 1-8 carbon atoms or benzyl; andSt is the residue of a steroid ABC ring system;Comprises reacting (a) a 17-oxo compound of the formula ##STR2## WHEREIN R.sub.1 and R.sub.2 are as defined above andSt* is said steroid ABC ring system residue, St, in a form which is chemically compatible with said reaction;With (b) an enolate ion of an alkoxyacetic acid alkyl ester of the formula ##STR3## wherein R.sub.3 and R.sub.4 are as defined above.