- A Br?nsted Acid Catalyzed Cascade Reaction for the Conversion of Indoles to α-(3-Indolyl) Ketones by Using 2-Benzyloxy Aldehydes
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A Br?nsted acid catalyzed, operationally simple, scalable route to several functionalized α-(3-indolyl) ketones has been developed and the long-standing regioisomeric issue has been eliminated by choosing appropriate carbonyls. A readily available and cheap bottle reagent was used as the catalyst. This protocol was also applicable to the synthesis of densely functionalized α-(3-pyrrolyl) ketones. A detailed mechanistic study confirmed the involvement of enolether as a reaction intermediate. Several postsynthetic modifications along with easy access to β-carboline, tryptamines, tryptophols, and spiro-indolenine proclaim the synthetic utility of this powerful building block. On the basis of this concept, functionalized carbazoles were constructed by a cascade annulation strategy.
- Banerjee, Ankush,Maji, Modhu Sudan
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supporting information
p. 11521 - 11527
(2019/08/16)
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- PEPTIDE, PEPTIDE ANALOG AND AMINO ACID ANALOG PROTEASE INHIBITORS
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Methods of use of compounds and compounds for the treatment of disorders characterized by the cerebral deposition of amyloid are provided. Among the compounds are those of formulae (I), (II) and (III): STR1 in which R. sub.1 is preferably 2-methyl propene, 2-butene, norleucine; R 2, R 4, and R 8 are each independently methyl or ethyl; R 3 is preferably iso-butyl or phenyl; R 5 is preferably iso-butyl; R 6 is H or methyl; R 7--(Q) n is preferably benzyloxycarbonyl or acetyl; Q is preferably--C(O)--; R B is preferbly iso-butyl; R A =--(T) m--(D) m--R 1, is which T is preferably oxygen or carbon, and D is preferably a mono-unsaturated C 3-4 alkenyl being more preferred; and X is an alcohol, particularly a secondary alcohol.
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- PEPTIDE AND PEPTIDE ANALOG PROTEASE INHIBITORS
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Methods of use of compounds and compounds for the treatment of disorders characterized by the cerebral deposition of amyloid are provided. Among the compounds are those of formulae I and II: STR1 in which R 1 is preferably 2-methyl propene, 2-butene, cyclohexyl or cyclohexylmethyl; R. sub.2, R 4, and R 8 are each independently methyl or ethyl; R 3 is preferably iso-butyl or phenyl; R 5 is preferably iso-butyl; R 6 is H or methyl; R 7--(Q) n is preferably benzyloxycarbonyl or acetyl; Q is preferably--C(O)--; R 8 is preferbly iso-butyl; R A =--(T) m--(D) m--R 1, is which T is preferably oxygen or carbon, and D is preferably a mono-unsaturated C 3-4 alkenyl being more preferred; and X is preferably an α-ketoester or α-ketoamide.
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- N- tripeptide derivatives as inhibitors of renin
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The following N-2(S)-hydroxy-4-methylpentyl derivatives of Gly-Val-Phe-OMe and Leu-Val-Phe-OMe were designed as analogues of the transition state of the renin-angiotensinogen reaction: N- Gly-Val-Phe-OMe 2 and N-2(S)-hydroxy-
- Quirante, Josefina,Johnson, Rodney L.
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- Synthesis and Chemical Properties of Tetrazole Peptide Analogues
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Tetrazole dipeptide analogues in which the amide bond is replaced with the tetrazole ring were synthesized from the corresponding Z or Pht protected dipeptide esters via the imidoyl chloride and imidoyl azide intermediates.Of the various imidoyl chloride/
- Yu, Kuo-Long,Johnson, Rodney L.
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p. 2051 - 2059
(2007/10/02)
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