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WO2010054961 Spiro-5,6-dihydro-4H-2,3,5,10B-tetraaza-benzo[E]azulenes
WO2010054961.pdf
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Biological target:
Vasopressin:
V1a
Activity:
antagonist
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Organic reaction
■ Palladium-catalyzed coupling reactions
►Buchwald-hartwig amination
►Fukuyama reaction
►Heck reaction
►Hiyama coupling
►Kumada coupling
►Liebeskind-Srogl coupling
►Negishi coupling
►Sonogashira reaction
►Stille reaction
►Suzuki reaction
■ Names reactions
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■ Multi-component reactions
►Biginelli reaction
►Bucherer-Bergs reaction
►Gewald reaction
►Hantzsch synthesis
►Mannich reaction
►Passerini reaction
►Strecker reaction
►Ugi reaction
■ Heterocycles
5-Membered rings
6-Membered rings
Fused rings
Organic synthesis
■ Protecting Groups
►Alcohol protecting groups
Ester
Ether
Ether silyl
►Amine protecting groups
Amine
Amide
Carbamate
Sulfonamide
►Carboxylic acid protecting groups
►Carbonyl protecting groups
■ Coupling Reagents in Peptide Synthesis
►Aminium
►Carbodiimides
►Phosphonium
►Uronium
►Other Couplig Reagents
■ Functional Group Synthesis
►Aldehydes
►Amides
►Amines
►Esters
►Halides derivatives
►Ketones
►Thioamides
■ Aminos acids
►Naturals aminos acids
►Homo aminos acids
►Beta-aminos acids
►Gamma-aminos acids
►Alkyls aminos acids
►Aryls aminos acids
Peptide synthesis
Patent Highlights
►Pfizer
WO2010035166
WO2010015972
WO2010016005
WO2010032200
WO2010007561
WO2010013161
WO2010038165
WO2010049841
WO2010052625
WO2010058314
WO2010058333
WO2010061329
WO2010038167
►Roche
WO2010020548
WO2010026110
WO2010043515
WO2010043513
WO2010018112
WO2010018113
WO2010026075
WO2010046273
WO2010028981
WO2010031708
WO2010031713
WO2010034649
WO2010034656
WO2010034657
WO2010034671
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WO2010040663
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WO2010049331
WO2010054961
WO2010054968
WO2010055004
WO2010055005
WO2010055006
WO2010030703
WO2010057795
WO2010063610
WO2010063634
WO2010031707
►Merck
WO2010022850
WO2010056717
WO2010056708
WO2010056496
WO2010056564
WO2010056567
WO2010056788
WO2010059773
WO2010062415
WO2010063352
WO2010065384
►Galapagos
WO2010010184
WO2010010186
WO2010010187
WO2010010189
WO2010029119
WO2010149769
►Astrazeneca
WO2010049731
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WO2010005385
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WO2010056194
WO2010055348
WO2010053438
WO2010049073
WO2010043893
WO2010039079
WO2010038081
WO2010038060
WO2010015849
►GSK
WO2010036831
WO2010045309
WO2010011818
WO2010022307
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WO2010011912
WO2010025087
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WO2010059774
WO2010059658
WO2010059555
WO2010059552
WO2010059549
WO2010062578
WO2010068262
WO2010135504
WO2010102958
►Novartis
WO2009158431
WO2010026122
WO2010026121
WO2010006191
WO2010007027
WO2010026124
WO2010015655
WO2010020675
WO2010007046
WO2010015628
WO2010029082
WO2010007120
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WO2010031750
WO2010043584
WO2010015613
WO2010002655
►Sanofi-aventis
WO2010000353
WO2010003624
WO2010004197
WO2010004198
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WO2010065571
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WO2010065803
WO2010070237
WO2010070238
►Janssen
WO2010000456
WO2010002774
WO2010008761
►Amgen
WO2010108074
WO2010126895
WO2010132589
Synthetic protocols
■ Functionals groups
Primary amine
Secondary amine
Aldehyde
Azido
Carboxylic acid
Cyanide
Epoxide
Ester
Ether
Hydroxyl
Ketone
Mesyl
Methoxy
Tosyl
Sulfonamide
■ Palladium-Catalyzed Coupling Reaction
Buchwald-Hartwig amination
Heck reaction
Negishi coupling
Sonogashira reaction
Stille reaction
Suzuki reaction
■ Protecting groups
N-Boc
N-Cbz
N-SEM
N-THP
N-TFA
N-DMPM
O-TBDMS
O-Bn
■ Coupling Reagents in Amide Synthesis
■ Multi-component reaction
Strecker reaction
Ugi reaction
■ Microwave synthesis
Alkyl amine synthesis
Buchwald-Hartwig amination
Cyanide synthesis
Ether synthesis
Stille reaction
Suzuki reaction
Thioether synthesis
Urea synthesis
■ Parallel synthesis
Reductive amination
Alkylation / deprotection / alkylation
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