- A concise and efficient synthesis of substituted morpholines
-
A simple and efficient method has been developed for the synthesis of substituted morpholines by a sequence of coupling, cyclization, and reduction reactions of easily available amino alcohols and α-halo acid chlorides. Various mono-, di-, and trisubstituted morpholines, spiro morpholines, and ring-fused morpholines, as well as morpholine homologues, were synthesized in good to excellent yields by a single methodology under similar reaction conditions. The method was also used in a multigram synthesis of (3S)-3-methylmorpholine.
- Dugar, Sundeep,Sharma, Amit,Kuila, Bilash,Mahajan, Dinesh,Dwivedi, Sandeep,Tripathi, Vinayak
-
supporting information
(2015/02/19)
-
- Trans-2-acylaminocyclohexyloxyacyldipeptides in the form of mixtures of diastereoisomers thereof and in the form of pure diasteredisomers, process for the preparation thereof and pharmaceutical compositions containing the same
-
There are described novel trans-2-acylaminocyclohexyloxyacyldipeptides of formula I STR1 wherein R1 represents --CO--R6, --SO2 --R7 or STR2 R6 is C1 -C18 alkyl or C1 -C18 alkoxy, R7 is C1 -C18 alkyl or an optionally substituted phenyl group, Y is =O, =S or =NH; R2 =R3 and represent --H or C1 -C12 alkyl, R4 represents --OR8 or --NHR9, R8 is --H, C1 -C8 alkyl or benzyl, R9 is --H, a straight or branched chain C1 -C18 alkyl group or benzyl group; R5 represents --OR9 or --NHR9, and novel (1R,2R)- and (1S,2S)-trans-2-acylaminocyclohexyloxyacetyldipeptides of the formulas Ia and Ib STR3 wherein R1 is --CO--R6, R6 is C1 -C18 alkyl, R2 is --H, R3 is --H or C1 -C12 alkyl, R4 is --OR8 or --NHR9, R8 is --H, C1 -C8 alkyl or benzyl, R9 is --H, C1 -C18 alkyl or benzyl, R5 is --OR9 or --NHR9 Compounds of formula I, Ia and Ib and the pharmaceutically acceptable alkali salts thereof show immunomodulatory and antitumour activities and can be used in the preparation of medicaments.
- -
-
-
- Preparation of diastereomerically pure immunologically active carbocyclic nor-muramyldipeptide analogues
-
The preparation of diastereomerically pure immunologically active carbocyclic nor-muramyldipeptide analogues (1'R,2'R)-/(1'S,2'S)-N-[2-(2'-acetylaminocyclohexyloxy)acetyl]-L- alanyl-D-isoglutamine and (1'R,2'R)-/(1'S,2'S)-N-[2-(2'-acetylaminocyclohexyloxy)acetyl]-L- alanyl-D-glutamic acid is described. The title compounds were synthesized using two independent synthetic routes from racemic trans-2-azidocyclohexanol and (1R,2R)-/(1S,2S)-2-aminocyclohexanol, respectively.
- Kikelj,Kidric,Pristovisek,Pecar,Urleb,Krbavcic,Honig
-
p. 5915 - 5932
(2007/10/02)
-
- A Convenient Synthesis of Trans-2-alkyl-octahydro-2H-1,4-benzoxazin-3-ones
-
Trans-octahydro-2H-1,4-benzoxazin-3-one and its 2-alkyl derivatives can be conveniently prepared from trans-2-azidocyclohexanol and corresponding α-haloacids.
- Gruevski, M.,Kidric, J.,Kikelj, D.,Krbavcic, A.,Pecar, S.,Urleb, U.
-
p. 2665 - 2676
(2007/10/02)
-