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1. A compound of formula I wherein R1 is —N(R3)R4; R2 is —OR21; R3 is:
H;C1-C6 alkyl optionally substituted with 1- to 3 R5;C2-C6 alkenyl optionally substituted with 1-3 R5;a 5- or 6-membered heteroaromatic ring selected from the group consisting of furanyl, pyridinyl, pyridinyl-N-oxide, pyrimidinyl, pyridazinyl, pyrazinyl, thiazolyl, triazinyl, thiadiazolyl, oxazolyl, isoxazolyl, triazolyl, each heteroaromatic ring being optionally substituted with 1-3 R30;imidazole fused with an aromatic or heteroaromatic ring selected from the group consisting of benzene, oxazole, isoxazole, furan, thiazole, pyrimidine, pyridine, pyrrole, pyrazine, thiophene, each aromatic or heteroaromatic ring being optionally substituted with 1 to 3 R30;benzo[1,3]dioxolyl;3H-isobenzofuran-1-onyl;cyano;C3-C6 alkynyl optionally substituted with 1-3 R5;—C(═O)R6;—C(═O)OCH2C(═O)R8;—C(═S)R6;—C(═S)NHR8;—C(═O)N(R8)R10;—OR7;—P(O)(OR15)2;—S(O)2R8;—SR8;—Si(R8)3;—N(R9)R10;—N═C(R15)R16;—(CHR22)mR37;—(CHR24)OR29; or—C(═NR16)SR16; or—C(═NR27)NR13R28; wherein m is an integer from 1-3; R4 is:
H;hydroxyl;amino;C1-C6 alkyl, optionally substituted with 1-3 R5;—C(═O)R6; or—C(═O)N(R8)R10; alternatively R3 and R4 may be taken together to form:
a 5- or 6-membered saturated or unsaturated ring containing 1-3 heteroatoms wherein each ring may be optionally substituted with 1-3 R11;═C(R12)N(R13)R14;═C(R13)(R14);═C(R15)OR15;═S(R34)2; or═NR35; R5 is independently halogen, C1-C6 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkylthio, C1-C4 haloalkylthio, amino, C1-C3 alkylamino, C2-C6 alkoxycarbonyl, C2-C6 alkylcarbonyl, C2-C6 alkylaminocarbonyl, —OH, N-methyl piperazine or C3-C6 trialkylsilyl; R6 is independently H, C1-C6 alkyl, C2-C6 alkenyl optionally substituted with 1-3 R30, C1-C5 haloalkyl, C1-C5 alkoxy, C1-C5 haloalkoxy C2-C6 alkoxycarbonyl, C1-C4 alkoxyalkoxy, C2-C6 alkylaminocarbonyl; 1-benzo[1,2,3]thiadiazol-7-yl, thiazolyl, benzyl, phenyl, phenoxy, or benzyloxy wherein the thiazolyl, benzyl, phenyl, phenoxy, or benzyloxy may be optionally substituted with 1-3 R20, or a 5- or 6-membered saturated or unsaturated ring containing 1-3 heteroatoms wherein each ring may be optionally substituted with 1-3 R11; R7 is H, C1-C6 alkyl, C2-C6 alkenyl, C1-C5 halo alkyl, benzyl which may be optionally substituted with 1-5 R20, —CHR18C(O)OR19, —(CHR27)R28, —Si(R8)3, or a 5- or 6-membered saturated or unsaturated ring containing 1-3 heteroatoms wherein each ring may be optionally substituted with 1-3 R11; R8 is independently C1-C6 alkyl, C1-C6 haloalkyl, amino, C1-C6 alkylamino, C2-C6 dialkylamino, methylene-2-furanyl, —CHR15C(O)OR19, benzyl optionally substituted with 1-3 R30, phenyl optionally substituted with 1-3 R30, or a 5- or 6-membered saturated or unsaturated ring containing 1-3 heteroatoms wherein each ring may be optionally substituted with 1-3 R11; R9 is H, C1-C6 alkyl C1-C6 haloalkyl, —C(═O)R17, benzothiazoyl, quinazolinyl, or phenyl optionally substituted with 1-3 R20, or a 5- or 6-membered saturated or unsaturated ring containing 1-3 heteroatoms wherein each ring may be optionally substituted with 1-3 R11; R10 is H or C1-C6 alkyl, C1-C6 haloalkyl, or phenyl optionally substituted with 1-3 R20; R11 is independently halogen, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, amino, C1-C6 alkylamino, C2-C6 dialkylamino, C2-C6 alkoxycarbonyl, or C2-C6 alkylcarbonyl; R12 is H or C1-C4 alkyl; R13 and R14 are independently H, cyano, —OH, C1-C4 alkyl, C1-C6 alkoxy, C2-C6, alkylcarbonyl, phenyl, or benzyl wherein the phenyl or benzyl may be optionally substituted with 1-3 R20; alternatively R13 and R14 may be taken together to form:
a 5- or 6-membered saturated or unsaturated ring containing 1-3 heteroatoms wherein each ring may be optionally substituted with 1-3 R11, or 3,4-dihydro-1H-isoquinolin-2-yl; alternatively R12 and R13 may be taken together to form:
a 5- or 6-membered saturated or unsaturated ring containing 1-3 heteroatoms wherein each ring may be optionally substituted with 1-3 R11; R15 is H or C1-C6 alkyl, C2-C6 alkenyl, 2-benzofuranyl, or a 5- or 6-membered saturated or unsaturated ring containing 1-3 heteroatoms wherein each ring may be optionally substituted with 1-3 R11; R16 is H, C1-C6 alkyl, or phenyl optionally substituted with 1-3 R20; alternatively R15 and R16 may be taken together as —(CH2)4— or —(CH2)5—; R17 is H, C1-C6 alkyl, C2-C6 alkenyl, C1-C6 haloalkyl, C1-C6 alkoxy, benzyl, phenyl, phenoxy, or benzyloxy wherein each ring may be optionally substituted with 1-3 R20, a 5- or 6-membered saturated or unsaturated ring containing 1-3 heteroatoms wherein each ring may be optionally substituted with 1-3 R11; R18 is H, C1-C6 alkyl, or C1-C6 haloalkyl; R19 is H, C1-C6 alkyl, C1-C6 haloalkyl, or benzyl; R20 is independently halogen, cyano, nitro, amino, C1-C6 alkoxyalkoxy, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 hydroxyalkyl, C2-C6 alkoxyalkyl, C2-C6 haloalkoxyalkyl, C2-C6 alkenyl, C2-C6 haloalkenyl, C3-C6 alkynyl, C3-C6 haloalkynyl, hydroxyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C2-C6 alkenyloxy, C2-C6 haloalkenyloxy, C3-C6 alkynyloxy, C3-C6 haloalkynyloxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfonyl, C2-C6 alkenylthio, C2-C6 haloalkenylthio, C2-C6 haloalkenylsulfonyl, C3-C6 alkynylthio, C3-C6 alkynylsulfonyl, C3-C6 haloalkynylsulfonyl, C1-C6 alkylamino, C2—CS dialkylamino, C3-C8 dialkylaminocarbonyl, C2-C6 alkoxycarbonyl, C2-C6 alkylcarbonyl, C3-C6 trialkylsilyl, 2-[(E)-methoxyimino]-N-methyl-acetamidyl, phenyl, benzyl, benzyloxy, phenoxy, or a 5- or 6-membered heteroaromatic ring wherein each phenyl, benzyl, benzyloxy, phenoxy, or 5- or 6-membered heteroaromatic ring may be optionally substituted with 1-3 substitutents independently selected from R31; R21 is:
H;C1-C4 alkyl;C1-C6 haloalkyl;C2-C4 alkenyl;C2-C4 haloalkenyl;C3-C4 alkynyl;C3-C4 haloalkynyl;phenyl, naphthyl, or tetrahydroquinolinyl each optionally substituted with 1-3 R20;—(CHR22)mR23;—(CHR24)mC(O)OR25;—(CHR24)mC(O)R26;—(CHR24)mC(O)N(R27)R28;—(CHR24)mOR29;—(CHR24)mSR29;—(CHR24)mN(R27)R28;—C(═O)R32;—N═C(R32)(R36);—NR25C(═O)OR25;—Si(R8)3;—SO2R33;C2-C6 alkoxy carbonyl;C2-C6 alkylaminocarbonyl;C2-C6 alkylcarbonyl;sugars selected from the group consisting of beta-D-glucose-tetraacetate, rhamnose, fructose, and pentose; ora 5- or 6-membered heteroaromatic ring selected from the group consisting of furanyl, pyridinyl, pyridinyl-N-oxide, pyrimidinyl, pyridazinyl, pyrazinyl, pyrazolyl, thiazolyl, triazinyl, thiadiazolyl, oxazolyl, triazolyl or isoxazolyl wherein each 5- or 6-member heteroaromatic ring may be optionally substituted with 1-5 R20; R22 is independently:
H;halogen;cyano;nitro;C1-C6 alkyl;C1-C6 haloalkyl;phenyl or benzyl optionally substituted with 1-3 R20;C1-C6 hydroxyalkyl;C2-C6 alkoxylalkyl;C3-C6 haloalkynyl;C2-C6 alkenyl;C2-C6 haloalkenyl;C3-C6 alkynyl;C1-C6 alkoxy;C1-C6 haloalkoxy;C1-C6 alkylthio;C1-C6 alkylamino;C2-C8 dialkylamino;C3-C6 cycloalkylamino;C4-C6 (alkyl)cycloalkylamino;C2-C6 alkylcarbonyl;C2-C6 alkoxycarbonyl;C2-C6 alkylaminocarbonyl;C3-C8 dialkylaminocarbonyl;C3-C6 trialkylsilyl;ring-fused heteroaromatic rings selected from the group consisting of benzothiophenyl, quinolinyl, isoquinolinyl, thieno[2,3-b]pyridyl, 1-methyl-1H-thieno[2,3-c]pyrazolyl, and benzoimidazolyl, wherein each of the rings may be further substituted with 1-3 R20; ora 5- or 6-membered heteroaromatic ring selected from the group consisting of furanyl, pyridinyl, pyridinyl-N-oxide, pyrimidinyl, pyridazinyl, pyrazinyl, thiazolyl, triazinyl, thiadiazolyl, oxazolyl, isoxazolyl, triazolyl and thienyl; R23 is:
H;halogen;C1-C6 alkyl;C1-C6 haloalkyl;C2-C6 dialkylamino;phenyl optionally substituted with 1-5 R20;ring-fused heteroaromatic rings selected from the group consisting of benzothiophenyl, quinolinyl, isoquinolinyl, thieno[2,3-b]pyridyl, 1-methyl 1H-thieno[2,3-c]pyrazolyl, benzofuranyl and benzoimidazolyl, 2,3-dihydrobenzofuran-2-yl, 4-methyl-4H-thieno[3,2-b]pyrrol-5-yl, 1-methyl-1H-indol-5-yl, imidazo[1,2-a]pyridin-2-yl, imidazo[2,1-b]thiazol-6-yl, benzothiazol-2-yl, benzo[b]thiophen-7-yl, and 1-methyl-1H-indazol-3-yl, wherein each of the rings may be further substituted with 1-3 R20;naphthyl;benzo[1,3]dioxolyl;pyrrolidinonyl;oxetanyl;C1-C6 alkylthio optionally substituted with 1-5 R20;a 5- or 6-membered saturated or unsaturated ring containing 1-3 heteroatoms wherein each ring may be optionally substituted with 1-3 R11; ora 5- or 6-membered heteroaromatic ring selected from the group consisting of furanyl, pyridinyl, pyridinyl-N-oxide, pyrimidinyl, pyridazinyl, pyrazinyl, pyrazolyl, thiazolyl, triazinyl, thiadiazolyl, oxazolyl, isoxazolyl, triazolyl, imidazolyl, thiophene-2-yl and thiophen-3-yl wherein each heteroaromatic ring may be optionally substituted with 1-3 R20; R24 is H, C1-C6 alkyl, C1-C6 alkoxy, benzyl, or phenyl wherein each of the benzyl or phenyl may be optionally substituted with 1-3 R20; R25 is H, C1-C6 alkyl, phenyl or benzyl optionally substituted with 1-3 R20; R26 is:
H;C1-C6 alkyl;C1-C6 alkoxy;phenyl optionally substituted with 1-3 R20; ora 5- or 6 membered heteroaromatic ring selected from the group consisting of furanyl, pyridinyl, pyridinyl-N-oxide, pyrimidinyl, pyridazinyl, pyrazinyl, thiazolyl, triazinyl, thiadiazolyl, oxazolyl, triazolyl and isoxazolyl; R27 and R28 are independently:
H;benzyl or phenyl wherein each of the benzyl or phenyl may be optionally substituted with 1-3 R20; ora 5- or 6-membered saturated or unsaturated ring containing 1-3 heteroatoms wherein each ring may be optionally substituted with 1-3 R11; R29 is:
H;C1-C6 alkoxyalkyl;benzyl, benzoyl, or phenyl wherein each of the benzyl, benzoyl, or phenyl may be optionally substituted with 1-3 R20; ora 5- or 6-membered saturated or unsaturated ring containing 1-3 heteroatoms wherein each ring may be optionally substituted with 1-3 R11; R30 is independently halogen, cyano, nitro, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 hydroxyalkyl, C2-C6 alkoxyalkyl, C2-C6 haloalkoxyalkyl, C2-C6 alkenyl, C2-C6 haloalkenyl, C3-C6 alkynyl, C3-C6 haloalkynyl, hydroxyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C2-C6 alkenyloxy, C2-C6 haloalkenyloxy, C3-C6 alkynyloxy, C3-C6 haloalkynyloxy, C1-C6 alkylthio, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfonyl, C2-C6 alkenylthio, C2-C6 haloalkenylthio, C2-C6 haloalkenylsulfonyl, C3-C6 alkynylthio, C3-C6 alkynylsulfonyl, C3-C6 haloalkynylsulfonyl, C1-C6 alkylamino, C2-C8 dialkylamino, C3-C8 dialkylaminocarbonyl, C3-C6 trialkylsilyl, thiazolyl, phenyl, pyrimidinyl, or pyridyl, wherein the thiazolyl, phenyl, pyridyl, or pyrimidinyl may be optionally substituted with 1-3 R20; R31 is independently halogen, cyano, nitro, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 hydroxyalkyl, C2-C6 alkoxyalkyl, C2-C6 haloalkoxyalkyl, C2-C6 alkenyl, C2-C6 haloalkenyl, C3-C6 alkynyl, C3-C6 haloalkynyl, hydroxyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C2-C6 alkenyloxy, C2-C6 haloalkenyloxy, C3-C6 alkynyloxy, C3-C6 haloalkynyloxy, C1-C6 alkylthio, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfonyl, C2-C6 alkenylthio, C2-C6 haloalkenylthio, C2-C6 haloalkenylsulfonyl, C3-C6 alkynylthio, C3-C6 alkynylsulfonyl, C3-C6 haloalkynylsulfonyl, C1-C6 alkylamino, C2-C8 dialkylamino, C3-C8 dialkylaminocarbonyl, or C3-C6 trialkylsilyl; R32 is independently:
C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 hydroxyalkyl, C2-C6 alkoxyalkyl, C2-C6 haloalkoxyalkyl, C2-C6 alkenyl, C2-C6 haloalkenyl, C3-C6 alkynyl, C3-C6 haloalkynyl, hydroxyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C2-C6 alkenyloxy, C2-C6 haloalkenyloxy, C3-C6 alkynyloxy, C3-C6 haloalkynyloxy, C1-C6 alkylthio, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfonyl, C2-C6 alkenylthio, C2-C6 haloalkenylthio, C2-C6 haloalkenylsulfonyl, C3-C6 alkynylthio, C3-C6 alkynylsulfonyl, C3-C6 haloalkynylsulfonyl, C1-C6 alkylamino, C2-C8 dialkylamino, C3-C8 dialkylaminocarbonyl, C3-C6 trialkylsilyl;phenyl wherein the phenyl ring may be optionally substituted with 1-3 R20; ora 5- or 6-membered saturated or unsaturated ring containing 1-3 heteroatoms wherein each ring may be optionally substituted with 1-3 R11; R33 is independently:
C1-C6 alkyl, C1-C6 haloalkyl, phenyl or thienyl optionally substituted with 1-3 R20, ora 5- or 6-membered saturated or unsaturated ring containing 1-3 heteroatoms wherein each ring may be optionally substituted with 1-3 R11; R34 is:
C1-C6 alkyl, C1-C6 haloalkyl, C2-C6 alkoxyalkyl, C1-C6 alkylamino; ora 5- or 6-membered saturated or unsaturated ring containing 1-3 heteroatoms wherein each ring may be optionally substituted with 1-3 R11; R35 is:
C1-C6 alkyl, C2-C6 alkylcarbonyl; ora 5- or 6-membered saturated or unsaturated ring containing 1-3 heteroatoms wherein each ring may be optionally substituted with 1-3 R11; R36 is H, cyano, C1-C6 alkyl, C1-C6 alkoxy, benzyl, or phenyl wherein each of the benzyl, or phenyl may be optionally substituted with 1-3 R20; alternatively R32 and R36 may be taken together to form:
a 5- or 6-membered saturated or unsaturated ring containing 1-3 heteroatoms wherein each ring may be optionally substituted with 1-3 R11; and R37 is independently:
H, halogen, or phenyl optionally substituted with 1-5 R20;C1-C6 alkyl, C1-C6 haloalkyl, hydroxyl, C1-C6 alkoxy, or C1-C6 haloalkoxy; ora 5- or 6-membered saturated or unsaturated ring containing 1-3 heteroatoms wherein each ring may be optionally substituted with 1-3 R11; wherein the compound of formula I must include at least one of the following substituents:
R3 is —C(═NR27)NR13R28;R4 is hydroxyl or amino;R6 is C2-C6 alkenyl optionally substituted with 1-3 R30;R7 is —(CHR27)R28, or —Si(R8)3;R8 is methylene-2-furanyl, —CHR15C(O)OR19, or benzyl optionally substituted with 1-3 R30;R9 is benzothiazoyl, quinazolinyl, or a 5- or 6-membered saturated or unsaturated ring containing 1-3 heteroatoms wherein each ring may be optionally substituted with 1-3 R11;R15 is C2-C6 alkenyl, 2-benzofuranyl, or a 5- or 6-membered saturated or unsaturated ring containing 1-3 heteroatoms wherein each ring may be optionally substituted with 1-3 R11;R17 is C2-C6 alkenyl, benzyl, or a 5- or 6-membered saturated or unsaturated ring containing 1-3 heteroatoms wherein each ring may be optionally substituted with 1-3 R11;R29 is benzoyl. |
