- Mild Base Promoted Nucleophilic Substitution of Unactivated sp3-Carbon Electrophiles with Alkenylboronic Acids
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Diverse alkenylboronic acids react smoothly with various sp3-carbon electrophiles such as unactivated alkyl triflates in the presence of mild bases such as K3PO4. The reaction protocol is very mild and thereby enables high functional group tolerance. This transition metal-free condition is orthogonal towards the classic transition metal catalyzed Suzuki coupling. (Figure presented.).
- Liu, Shiwen,Zeng, Xiaojun,Hammond, Gerald B.,Xu, Bo
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supporting information
p. 3667 - 3671
(2018/09/12)
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- CARBOXYLIC DERIVATIVES FOR USE IN THE TREATMENT OF CANCER
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The invention provides novel compounds of formula (I), wherein: R1 is a radical derived from one of the known ring systems; R2 is a phenyl radical optionally substituted; Xn represents a birradical selected from the group consisting of: -(CH2)1-4-, (C2-C4)-alkenyl, (C2-C4)alkynyl, -S-(CH2)1-3-#, and -(CH2)1-3-O-#; wherein the symbol # indicates the position at which Xn is attached to R1; Yn is a birradical selected from the group consisting of: -(CH2)2-4-, -S-(CH2)1-3#, and -O-(CH2)1-3-#,; where in the symbol # indicates the position at which Yn is attached to R2; and R3 is a radical selected from the group consisting of: -OR4. The compounds of formula (I) are useful in the treatment of cancer
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Page/Page column 94
(2009/07/25)
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- Process for the preparation of N-alkylated dipeptides and their esters
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The invention relates to a process for the preparation of compounds of the formula I STR1 in which n is 1 or 2, R represents hydrogen, an aliphatic, cycloaliphatic, aromatic, araliphatic, cycloaliphatic-aliphatic radical or a radical ORa or SR2, in which Ra denotes alkyl, aryl or heteroaryl, R1 denotes hydrogen, an aliphatic, cycloaliphatic-aliphatic, aromatic, araliphatic, heteroaromatic radical or an aminoacid side chain, R2 and R3 are identical or different and denote hydrogen, an aliphatic, cycloaliphatic, aromatic or araliphatic radical, and R4 +R5, together with the atoms carrying them, form a heterocyclic ring system, which comprises reacting trifluoromethanesulfonic acid derivatives of the formulae II or III with aminoacid esters of the formulae IV or V respectively. The invention also relates to compounds of the formula III and a process for their preparation.
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- A FAVOURABLE DIASTEREOSELECTIVE SYNTHESIS OF N-(1-S-ETHOXYCARBONYL-3-PHENYLPROPYL)-S-ALANINE
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N-(1-S-Ethoxycarbonyl-3-phenylpropyl)-S-alanine is prepared by Michael addition of S-alaninebenzylester to ethyl-4-oxo-4-phenyl-2-butenoate in a regio- and diastereoselective fashion and subsequent catalytic hydrogenolysis.
- Urbach, H.,Henning, R.
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p. 1143 - 1146
(2007/10/02)
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