公开(公告)号：US3558683A

公开(公告)日：1971-01-26

申请号：US3558683D

申请日：1967-03-20

Applicant: YISSUM RES DEV CO

Inventor： BELSKY IGAL ,  GERTNER DAVID ,  ZILKHA ALBERT

IPC: C07F7/08 ,  C07F7/02

CPC classification number: C07F7/0818 ,  C07F7/0812

Abstract: AMIDES, UREIDES, THIOUREIDES AND GUANIDINE DERIVATIVES OF THE FOLLOWING GENERAL FORMULA, AND TO PROCESSES FOR THE PREPARATION OF THESE COMPOUNDS.

(R1-SI(-R2)(-R3)-(CH2)I-),(R4-CO-(CH2)N-)BENZENE

WHEREIN THE BENZENE RING IS SUBSTITUTED IN THE ORTHO, META OR PARA POSITION BY RADICAL CONTAINING A TRI-SUBSTITUTED SILYL GROUP (R1R2R3SI), R1,R2, AND R3 ARE ALKYL OR ARYL GROUPS, SAME OR DIFFERENT HAVING UP TO 10 CARBON ATOMS, N IS ZERO OR A WHOLE NUMBER FROM 1 UP TO 10, R4 IS A RESIDUE OF AMMONIA, HYDROXYLAMINE, HYDRAZINE OR N-ALKYL OR ARYL SUBSTITUTED HYDRAZINE, OR A PRIMARY OR A SECONDARY AMINE WHETHER SUBSTITUTED OR UNSUBSTITUTED, ALIPHATIC AROMATIC OR HETEROCYCLIC, OR THE RESIDUE OR UREA, THIOUREA OR GUANIDINE, OR THEIR SUBSTITUTED DERIVATIVES, ALL SAID RESIDUES BEING CONNECTED THROUGH NITROGEN TO THE C=O GROUP; I IS ZERO OR ONE. THESE MATERIALS SERVE AS CENTRAL NERVOUS SYSTEM DEPRESSANTS.

公开(公告)号：US3505376A

公开(公告)日：1970-04-07

申请号：US3505376D

申请日：1965-10-22

Applicant: YISSUM RES DEV CO

Inventor： FRANKEL MAX ,  GERTNER DAVID ,  BROZE MORDECHAI ,  HANNA PARDESS ,  ZILKHA ALBERT

IPC: C07F7/08 ,  C07F7/10

CPC classification number: C07F7/0818

Abstract: Novel trialkylsilyl-b -phenylethylamine compounds having the formula wherein R1, R2 and R3 are alkyl, R4 is hydrogen, hydroxyl or alkyl, R5 is hydrogen, hydroxymethyl, carboxyl or alkyl, R6 and R7 are hydrogen or alkyl and when R6 is hydrogen then R7 may also be acyl or haloacyl, are prepared from intermediates of formula where n is 0 or 1, X is chlorine, carboxyl, nitrile or hydroxyl and R8 is hydrogen, alkyl or acyl. In examples preparations described are of b - (trimethylsilylphenyl)ethylamine from trimethylsilylbenzyl cyanide and lithium aluminium hydride; b -(trimethylsilylphenyl)ethyldimethylamine from b -(trimethylsilylphenyl)-ethyl chloride and dimethylamine; b -(trimethylsilylphenyl)-propylamine from a -(trimethylsilylphenyl)propionitrile and lithium aluminium hydride; 1-(trimethylsilylphenyl)-2-aminopropane by reacting trimethylsilylbenzyl cyanide with magnesium, then with methylcyanide and reducing with lithium aluminium hydride; b -(trimethylsilylphenyl) -serine from trimethylsilylbenzaldehyde and glycine; 1-(trimethylsilylphenyl)-2-aminopropane-1,3-diol from b -(trimethylsilylphenyl)serine and lithium aluminium hydride; 1 - (trimethylsilylphenyl) - 2 - dichloroacetamido propane-1,3-diol from the -2-aminopropane-1,3-diol and methyl dichloracetate. Intermediates, other than those used as starting materials above, which are prepared are trimethylsilylphenyl acetic acid, b -(trimethylsilylphenyl) ethyl alcohol, trimethylsilylbenzyl chloride and 1-cyano-1-(trimethylsilyl)-phenyl acetone. The methods of preparing the intermediates are described.

公开(公告)号：US3651115A

公开(公告)日：1972-03-21

申请号：US3651115D

申请日：1967-05-18

Applicant: YISSUM RES DEV CO

Inventor： BELSKY IGAL ,  GERTNER DAVID ,  ZILKHA ALBERT

IPC: C07F7/08 ,  C07F7/10

CPC classification number: C07F7/0818 ,  Y10S514/818

Abstract: COMPOUNDS OF THE FORMULA

(R4-C(-R5)(-OH)-CH(-CO-R6)-),(R1-SI(-R2)(-R3)-)BENZENE

WHEREIN R1,R2, AND R3 ARE ALKYL OR ARYL; R4 AND R5 ARE HYDROGEN, ALKYL, ARALKYL,, OR FORM TOGETHER WITH THE ADJOINING CARBON ATOM CARRYING THE HYDROXYL GROUP A CYCLOHEXYL, CYCLOPENTYL OR CYCLOHEPTYL GROUP; AND R6 IS HYDROXYL, A RESIDUE OF AN ALCOHOL CONNECTED THROUGH ITS HYDROXYL GROUP TO THE CARBONYL GROUP BY AN ESTER LINKAGE AND CONTAINING A TERTIARY AMINO GROUP AND HAVING AN ALKYL OR CYCLOALKYL OR HETEROCYCLIC OR A CONDENSED BIHETEROCYCLIC SKELETON, OR IS A RESIDUE OF ANY OF AMMONIA, HYDROXYLAMINE, HYDRAZINE, N-ALKYL OR ARYL SUBSTITUTED HYDRAZINE, A PRIMARY OF SECONDARY AMINE, UREA, THIOUREA OF GUANIDINE OR THEIR SUBSTITUTED DERIVATIVES, ALL OF SUCH RESIDUES BEING CONNECTED THROUGH NITROGEN TO THE C=O GROUP. THE COMPOUNDS DISPLAY ANTI-CHOLINERGIC ACTIVITY AND ARE ANTIDOTAL AGAINST ORGANO-PHOSPHATE POISONING.

公开(公告)号：US3426002A

公开(公告)日：1969-02-04

申请号：US3426002D

申请日：1965-05-12

Applicant: YISSUM RES DEV CO

Inventor： FRANKEL MAX ,  GERTNER DAVID ,  WAGNER DANIEL ,  ZILKHA ALBERT

IPC: C08G79/12 ,  C08G17/00

CPC classification number: C08G79/12