1 -Benzyl-2,4-dialkyl-5-hydroxy-methyl

Cyclocondensation of pipecolinic acid and malic acid anhydride in pyridine afforded 3-hydroxy-2,3-dimethylperhydropyrido[l,2-a]pyrazine-l, 4-dione (74CB2804). Cyclocondensation of bis(2,4,6-trichlorophenyl) mal-onates with 2-methyl-, 2-benzyl- and 2-ethoxycarbonylmethylquinoxalines and -3-ones at 250°C afforded 8-hydroxy-10//-pyrido[l,2-a]quinoxalin-10-ones and their 5,6-dihydro-6,10-dione derivatives (77M103). Under Horner-Wittig reaction conditions, the reactions of 2-formylquinoxaline and dialkyl phosphonosuccinates (314) also involved cyclization to give alkyl 10-oxo-10//-pyrido[l,2-a]quinoxahne-8-carboxylate (80LA542). 

C-Trapping. Alkylation or hydroxy alkylation (i.e., reaction with RCHO) of enolates derived from conjugate addition of organocuprates affords vicinal dialkylated products. However, the reaction is confined to highly reactive alkylating agents such as methyl, allyl, propargyl, benzyl, and a-halocarbonyl compounds or aldehydes. 

Dialkyl-4,5,6,7-tetrahydro- 311 2-Hydroxy-5-(2-methylamino-l-hydroxy-athyl)- 208 2- Hydroxy- 5-( N- methyl-N-benzyl-aminoacetyl)-... 

Dialkyl dimethyl ammonium chloride Dialkyl methyl benzyl ammonium chloride Dicapryl sodium sulfosuccinate Dicoco methylamine Didecyidimonium chloride Diethylaminoethyl cocoate Diethylaminoethyl PEG-5 cocoate Diethylaminoethyl stearate Di(hydrogenated tallowalkyl) methyl (2-hydroxy-2-methylethyl) ammonium chloride Dihydroxyethyl C12-15 alkoxypropylamine oxide... 

We made an effort to set up a synthetic method for the preparation of two enantiomers of chiral 1-(substituted phenoxyacetoxy)aIkylphosphonates by the condensation of substituted phenoxyacefyl chlorides MS and optically pure 1-hydroxyl-1-(substituted benzyl)phosphonates M2. At this stage, three series of novel (5,(5-dialkyl 1-(substituted phenoxyacetoxy)- -(substituted phenyl)methyl-phosphonates lA, IE, and IF including 78 (14 lA, 16 IE and 48 IE) optically active isomers were successfully prepared in higher enantiomeric excess (ee) under the Schotten-Baumann conditions. The stmctures of these optically active compounds were characterized by and NMR, IR, and MS, and were confirmed by elementary analysis. The absolute configurations of these optically active products I A, IE, and IF originated from the configurations of optically active reactant, 1-hydroxy(substituted phenyl)methylphosphonates M2. The enantiomeric excesses (ee) of lA, IE, and IF were reduced just a little compared with those of chiral 1-hydroxy(substituted phenyl)methylphosphonates M2. 

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