2- -2-oxoethyl

Oxoethyl)-2-cycloalken-l-ones, 57,117 4-OXOHEXANOIC ACID ETHYL ESTER,... 

Methyl (2i )-l-(ferf-Butoxycarbonyl)-2-(2-oxoethyl)pyrrolidine-2-carboxylate (83) [m ... 

Michael/Henry/dehydration/aromatisation reaction of 2-(2-oxoethyl) benzal-dehydes and nitroalkenes mediated by pyrrolidine to obtain polysubstituted naphthalene derivatives. DBU catalysed the conjugate additions of alcohols to ot,p-unsaturated nitriles, esters and ketones. Perhaps more important are the aza-Michael addition reactions of amines to a,p-unsaturated ketones, nitriles and esters. Recently, Costa, Vilarrasa and coworkers described the addition of lactams, imides, 2-pyridone, pyrimidine-2,4-diones and inosines to methyl propiolate and other similar compounds, DABCO and DMAP being the best catalysts. As mentioned before, tertiary amines give zwitterionic species with activated allynes. It was as early as 1932 when Diels and Alder used the reaction of pyridine with dimethyl acetylenedicarbojylate (DMAD) for the synthesis of heterocycles. The interception of the corresponding intermediate with Al-tosylimines and activated olefins provided access to l-azadienes ° and highly substituted butadienes (Scheme 2.6). When the quenching species of the zwitterionic intermediate is a 1,2-diketone, dibenzoyl maleates or cyclopentenedione derivatives could be obtained (Scheme 2.6). The interception of the zwitterionic species of N-methyl imidazole (NMI) and DMAD with ketenes to obtain unsaturated esters has also been shown. ... 

Prefixes that represent complete terminal characteristic groups are preferred to those representing only a portion of a given group. For example, for the prefix — C(=0)CH3, the name (formylmethyl) is preferred to (oxoethyl). 

Benzoic acid-3,6-dichloro-2-methoxy-2-ethoxy-l-methyl-2-oxoethyl ester [87214-73-1]... 

Carboxyl group of (-)-9-fluoro-3-methyl-7-oxo-10-[(3S)-3-(tert-butoxy-carbonylamino)pyrrolidino]-2,3-dihydro-7//-pyrido[l,2,3- 7e]-l,4-benzoxa-zine-6-carboxylic acid was converted into l-nitro-2-oxoethyl group in 45% yield by treatment with l,l -carbonyldiimidazole in boiling CFICI3 for 18h, then with MeN02 in the presence of KOr-Bu for another 18 h (96MI12). 6-(2,2-Diethoxycarbonyl)acetyl derivative formed from the aforementioned 6-carboxylic acid, when it was treated with l,l -carbonyldiimidazole in... 

Reduction of a 7-(2-oxoethyl) derivative with NaBH4 in EtOH at room temperature gave 7-(2-hydroxyethyl)-2-(2-pyrimidinyl)perhydropyrido[l, 2-u]pyrazine (99MIP6). Reduction of 7-formyl-8-[(4-cyanophenyl)methoxy]-1,3,4,6,11,1 lu-hexahydro-2//-pyrazino[l,2-A]isoquinoline-l,4-dione with NaBH4 yielded a 7-hydroxymethyl derivative (98MIP7). 

Hydroxy group of rru -7,9u-H-7-(prepared from 7-formyl-2-(2-pyrimidyl)perhydropyrido[l,2-u]pyrazine by the treatment with MeOCH2P(Ph)3Cl in the presence of -Pr2NH in THF at 0°C, than with BuLi at room temperature (99MIP6). 

The N,N -dibenzyl-N,N -bis-[2-(3, 4 -dihydroxyphenyl)-2-oxoethyl] -hexamethylene-diamine-dichlorohydrate-monohydrate used as the starting material was prepared as follows 2 mols of chloroaceto pyrocatechin were dissolved in 2,000 cc of acetone and heated to boiling with 2 mols of N,N -dibenzylhexamethylene-diamine for 12 hours, almost the theoretical quantity of N,N -dibenzylhexamethylene-diamine-dichlorohydrate being precipitated and removed by suction after cooling. Excess HCI was added to the filtrate, approximately 66% of the theoretically possible quantity of crude dichlorohydrate of the N,N -dibenzyl-N,N -bis-[2-(3, 4 -dihydroxyphenyl)-2-oxoethyl] -hexamethylene-diamine being precipitated. The product was cleaned by recrystallization from water with the addition of animal charcoal. After drying the substance contained water of crystallization at ambient temperature, MP 206° to 209.5°C. 

Two low-molecular weight initiators with azo groups of different stability were used by Simionescu et al. [82,83] for polymerizations phenylformamidoethyl 4-/-butylazo-4-cyanovalerate (Scheme 20) and N,N -bis[(4-t-butylazo-4-cyanovaleryl)-oxoethyl]azo-bis-form-amide (Scheme 21) [84-86]. 

Dimethyl (7RS,12RS,8EZ,13EZ)- and (7/TS J2.VOEZJ3 Z)-7,12-Bis 2-(dimethylamino>-2-oxoethyll-... 

Aldol Reaction of (4R,5,5)-3-(2-cliloro-l-oxoethyl)-4-inefliyl-5-phcnyl-l,3-oxazolidin-2-one Typical Procedure ... 

An entry to. yyrt-2-methoxy-3-hydroxycarboxylic acids is also opened using similar methodology. Thus the norephedrine derived (4/ ,5S)-3-(2-methoxy-l-oxoethyl)-4-methyl-5-phenyl-1,3-oxazolidine-2-one 23105a, as well as the phenylalanine derived (4S)-4-benzyl-3-(2-methoxy-l-oxoethyl)-l,3-oxazolidin-2-one 25105b, can be added to aldehydes via the boron enolates to give, after oxidative workup, the adducts in a stereoselective manner (d.r. 96 4, main product/sum of all others). Subsequent methanolysis affords the methyl esters. 

R = CH2Si(CH3)3 xam-4-[2-(4-methylphenyt)-2-oxoethyl -3-phih.alimido-l-lrimethylsihlmeihyl-2-aze-tidinone106 yield 70 % mp 175 -177 °C... 

R = 4-CH3OC6H4 . Tans-1-(4-methoxypheny[)-4-[2-(4-methylphenyl)-2-oxoethyl -3-phthalimido-2-aze-tidinone ob yield 40% mp 143-145°C... 

Y2 receptors are characterised by an order of potency of NPY PYY > C-terminal fragment [Pro34]-substituted analogue > PP. BIIE 0246 ((S -iV2- 1 -[2-[4-[(i ,5)-5,11 -dihydro-6(6h)-oxodibenz[b,e]azepin-l 1 -yl]-l-piperazinyl]-2-oxoethyl]cyclopentyl]acetyl]-iV -[2-[l, 2-di-hydro-3,5-(4H)-dioxo-l, 2-diphenyl-3H-l, 2,4-ttiazol-4-yl]ethyl]-argininamide) is a Y2-selective antagonist with an affinity of 3 nM. 

Alkylzinc halides have also been prepared under microwave irradiation. The Reformatsky reagents (2-t-butoxy-2-oxoethyl)zinc bromide and [(2-dibenzylamino)-2-oxoethyl]zinc bromide were synthesized from the corresponding bromides via reaction with zinc in THF (Scheme 5) [24], The oxidative addition was executed at 100 °C in 5 min. The obtained reagents were subsequently used in Negishi reactions on 2-bromopyridine, 3-bromopyridine, 2-bromo-5-nitropyridine, and 2-bromo-5-trifluoromethyl-pyridine using Pd(PPh3)4 as a catalyst (Scheme 5). 

Inhibitors for proteases plasmepsin I and II of the malaria parasite Plasmodium falciparum, with a good plasmepsin/human protease cathepsin D selectivity, have been identified via library construction involving rapid microwave-accelerated Suzuki reactions [57]. The phenyl ring of the biphenyl unit in the lead compound M-((lS)-l- [((lS,2S)-3- [(lS)-2-amino-l-(4-phenyl-benzyl)-2-oxoethyl]amino -2-hydroxy-l-phenoxypropyl)amino]carbonyl -2-methylpropyl)pyridine-2-carboxamide has been altered by performing Suzuki reactions on N-((lS)-l- [((lS,2S)-3- [(lS)-2-amino-l-(4-bromobenzyl)-2-oxoethyl]amino -2-hydroxy-l-phenoxypropyl)amino]carbonyl -2-methyl-propyl)pyridine-2-carboxamide (Scheme 37). In particular, a 2-benzofuryl moiety proved to be interesting since a Ki value of 13 nM for plasmepsin I and... 

CN 4-[[4-[(aminoiminomethyl)amino]benzoyl]oxy]benzeneacetic acid 2-(dimethylamino)-2-oxoethyl ester monomesylate... 

CN [3(S)-endo,a /i]-8-(2-ll,r-biphenyl]-4-yl-2-oxoethyl)-3-(3-hydroxy-l-oxo-2-phenylpropoxy)-8-methy 8-azoniabicyclo[3.2.1]octane bromide... 

CN yV-[3 Chloro-2-[[methyl[2-(4-morpholinyl)-2-oxoethyl]aminoJmethyl]phenyl]benzamide... 

CN 7-[(aminoiminomethyl)amino]-A(-[2-[[4-[(3-aminopropyl)amino]butyl]amino]-1 -hydroxy-2-oxoethyl]heptanamide... 

RN 53943-88-7 MF CioH,7N04S2 MW 279.38 EINECS 258-879-3 CN 2-[2-[(2-ethoxy-2-oxoethyl)thio]ethyl]-4-thiazolidinecarboxylic acid... 

CN (5)-2-Ethoxy-4-[2-[[3-methyl-l-[2-(l-piperidinyl)-phenyl]butyl]amino]-2-oxoethyl]benzoic acid (S)-(+)-Ca salt... 

C ,H jN5Na04S 35334-12-4) see Bacampicillin 17a-azido-3P,16a-diacetoxy-5a-pregnane-ll,20-dione (C25H35NtiO 5167-90-8) see Deflazacort Fluazacort 2-azido-7V-[2-(2,5-dimcthaxyphenyl)-2-oxoethyl]acetamide (C,2H,4N404 59939-34-3) see Midodrine 2-azidoethanol... 

C H2 C103 76811-97-7) see Fexofenadine hydrochloride 4-(2-chloro-2-oxoethyl)-l-piperidinecarboxylic acid phe-nylmethyl ester... 

C4H7Br 7051-34-5) see Betaxolol Ciraetropium bromide Flutoprazepam Naltrexone Prazepam A -cyclopropylmethyI-6,14-e do-ethano-7a-I(lS)-l-hy-droxy-1,2,2-trim ethylpropyijtetrahydronorthebaine (C30H43NO4 16524-65-5) sec Buprenorphine (2-cyc)opropyl-2-oxoethyl)triphenyIphusphomum bromide... 

CiiHijNOj I2I-2H-8) see Isoprenaline 7-[2-[2-[(3,4-dihydraxyphenyl)-2-oxoethyl](phenylme-thyl)amino]ethyl]-3,7-dihydro-l,3 dimethyl-l/f-purin-2,6-dione... 

Migchielsen MHJ (2004a) 8-Oxa-3,5-dithia-4-stannatetra-decanoic acid, 10-ethyl-4-[[2-(2-ethylhexyl)oxy]-2-oxoethyl]thio]-... 

Migchielsen MHJ (2004b) 8-Oxa-3,5-dithia-4-stannatetra-decanoic acid, 10-ethyl-4-[[2-(2-ethylhexyl)oxy]-2-oxoethyl]thio]-4-octyl-7-oxo-, 2-ethylhexyl ester [Mono-octyltin tris(2-ethyl-hexylmercaptoacetate), CAS No. 27107-89-7] 96-hour acute toxicity in zebra-fish with MOT(EHMA) (semi-static). TNO, Delft, for NOTOX, s-Hertogenbosch, 3 September (NOTOX Project 374985 TNO Study No. 5311/01). 

The 7-(2-oxoethyl) derivative was prepared from 7-formyl-2-(2-pyrimidyl)perhydropyrido[l,2- ]pyrazine by the treatment with MeOCHzP(Ph)3Cl in the presence of Pr 2NH in THF at 0°C, then with BuLi at room temperature < 1999WO99/020622>. Reaction of a 7-mesyloxymethyl group in perhydropyrido[l,2-tf Ipyrazine with NaCN in DMF at 110°C gave a 7-cyanomethyl derivative, which was converted into a 2-oxoethyl group by treatment first with DIBAL-H, then with 2M HC1. The 2-oxoethyl group was reacted with 4-FC6H4MgBr in THF at — 10°C to yield a... 

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