2-Methyl-l-methylamino

J ,3J ,4J ,5J )-2,5-bis(benzyloxy)-3,4-dihydroxy-Nd -bis (lS)-2-methyl-l-[(methylamino)carbonyl]propyl hexanediamide is a C2-symmetric HIV-1 protease inhibitor [29]. Derivatization in the para positions of the benzyl-oxy groups via microwave-assisted Stille reaction on the corresponding di-brominated inhibitor smoothly yielded the desired heteroarylated derivatives (Scheme 10). Interestingly, the 1,3-thiazole derivative showed a higher antiviral activity on the wild type virus than the lead compound. The activity remained at the same level in the presence of seriun. Unfortimately, a low activity was observed on mutants. 

H3C-NH2 elektrocfaemiacli an Hg-Kathode C2H50H/HC1/H20 pH 10-11, 10° 2-Methyl-l-methylamino- cyclohexan 80 2... 

Ethyl 3-bromomethyl-6,7-difluoro-2-quinoxalinecarboxylate 1,4-dioxide (84) gave 6-fluoro-2-methyl-7-methylamino-2,3-dihydro-17/-pyrrolo[3,4-h]quinoxalm-l-one 4,9-dioxide (85) (MeCN, MeNH2i, 15°C, 90 min 87% note additional replacement of one fluoro substituent) analogs likewise. ° ... 

CN cw-5-chloro-2-methoxy-4-(methylamino)-A-[2-methyl-l-(phenylmethyl)-3-pyrrolidinyl]benzamide... 

Chemical/Physical. Aminocarb was hydrolyzed in purified water to 4-(dimethylamin-o)-3-methylphenol before yielding o-methylbenzoquinone. This compound then oxidized to 6-(di-methylamino)-2-methyl-1,4-benzoquinone, 6-(methylamino)-2-methyl-l,4-benzoquinone, 5-(di-methylamino)-2-methyl-1,4-benzoquinone, and 5-(methylamino)-2-methyl-l,4-benzoquinone... 

Bromo-N-[4-chloro-2-methyl-6-[(methylamino)Carbonyl]Phenyl]-l-(3-chloro-2-pyridinyl)-1H- pyrazole-5-carboxamide... 

Methyl-l -methylamino-2-oxo-1,2-dihydro- IV/5b, 1299 Propinsaure Phenyl- -(2,2-dimethyl-hydrazid) E5, 1157 (OH - NH-NH2)... 

SYNS ISOMETHEPTENE 6-METHYLAMINO-2-METHYLHEPTENE METHYLISOOCTENYLAMINE 2-METHYL-6-METHYLAMINO-2-HEPTENE METHYL-OCTENYLAADNE OCTANIL OCTTN OCTINUM OCTON N-l,5-TRIMETHYL-4-HEXENYLAMINE... 

Methylamino-1 -( 2-chlor-phenoxy)- 451 2-Methyl- l-(2-amino-cyclohexyl)- l-furyl-(2)- 441 2-Methylamino- l-(N-cyclopropyl-benzylamino)- 452 2-Methylamino- l-(2,4-dichlor-phenoxy)- 451 2-Methylamino- l-methylimino-2-methyl- 1-phenyl-233... 

Methylamino- 1-phenyl- 98, 450 2-Methylamino-2-phenyl- 422, 495 2-Methyl-l-furyl-(2)- 335, 341 2-Methyl-1-tetrahydrofuryl-(2)- 335 2-Nitro-2-phenyl- 422, 495 2-Oxo- 1,3-diphenyl- 216... 

Methyl-l-athyl- 94 Methylamino- 418 4-Methyl-l-tert.-butyl- 84 cis-2-Methy l-1-carboxy-... 

The ring-contraction of the 4,6-diimino-5//-l,2,5-thiadiazine (12) (see Section 6.15.7) in the presence of a trace of hydroxide or cyanide ion involves a rare example of a nucleophilic attack on the 1,2,5-oxadiazine or 1,2,5-thiadiazine ring systems <79TL1281>. The product, which is also formed on treating 3-methylamino-2-methyl-l,2,5-thiadiazolium chloride ((91) see Section 6.15.7) with an excess of cyanide ion, is thought to be the imidazoline-2-thione (31) formed as indicated in Scheme 4, although an alternative cyclization of intermediate (30) to give the isomeric 2,4,5-tri-iminothiazolidine (32) is not discounted. 

Urea has been used successfully to convert 4-aminoimidazole-5-car-boxamide (and its derivatives) to purine-2,6-diones (see 19)124>202 2-amino-,250,251 2-methylamino-,252 and 2-anilinobenzamides253 to quinazo-line-2,4-diones (see 1) 3-aminopyrazolo-4-carboxamide118 and 4-aminopy-razole-3-carboxamide221 to the related pyrazolopyrimidinediones (see 16 and 17) and 4-amino-1- and 4-amino-2-methyl-l,2,3-triazole-5-carboxa-mides to 8-azapurine-2,6-diones (see 21).254... 

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