- Rhodacyclopentanones as Linchpins for the Atom Economical Assembly of Diverse Polyheterocycles
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We outline a conceptual blueprint that provides direct and atom economical access to a wide range of complex polyheterocycles. Our method capitalizes on the ambiphilic reactivity of rhodacyclopentanones that arise upon exposure of cyclopropanes to Rh(I) catalysts and CO. Using this approach, a wide array of polycyclizations are achieved, including variants that involve powerful dearomatizations and medium ring formations.
- Wang, Gang-Wei,Boyd, Olivia,Young, Tom A.,Bertrand, Sophie M.,Bower, John F.
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- 1,1a,6,6a-tetrahydrocycloprop[a]indene-1-amine derivatives and preparation method and applications thereof
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The invention belongs to the technical field of medicine, and discloses a 1,1a,6,6a-tetrahydrocycloprop[a]indene-1-amine derivative which is represented as formula (I) and a preparation method and applications thereof. The 1,1a,6,6a-tetrahydrocycloprop[a]indene-1-amine derivatives provided by the invention has good inhibitory activity against LSD1, has good selectivity for homologous enzymes suchas monoamine oxidase and LSD2, and is expected to develop into therapeutic medicine for diseases such as acute myeloid leukemia.
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Paragraph 0251; 0256; 0257; 0258; 0259
(2019/04/10)
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- NON-NUCLEOTIDE REVERSE TRANSCRIPTASE INHIBITORS
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Compounds of the formula Z: where; A is CH or N; R1 is a substituent to a carbon atom in the ring containing A selected from -S(=O)pRa, where Ra is -C1-C4 alkyl, -ORx, -NRxRx, -NHNRxRx, - NHNHC(=O)ORx, -NRxOH; -C(=O)-Rb, where Rb is -CT-C4-alkyl, ORx, -NRxRx, -NHNRxRx, -NHC1-C3-alkyl-C(=O)Orx -NRxRc, where Rc is H, C1-C4 alkyl, -NRxRx; -C(=0)Rd, -CN, S(=O)pRx where Rd is Rd is C1-C4-alkyl, -ORx, -NRxRx C1-C3-alkyl-O-Cl-C3alkylC(=O)ORx, -C1-C3-alkyl-COORx; -C1-C3alkyl-OH or C1-C4 alkyl ethers or esters thereof (O-Cl-C3alkyl)q-O-Rx a 5 or 6 membered aromatic ring having 1-3 hetero atoms p is 1 or 2; Rx is independently selected from H, C1-C4 alkyl or acetyl; or a pair of Rx can together with the adjacent N atom form a ring; L is -0-, -S(=O),- or -CH2-, where r is 0, 1 or 2; R3-R7 are substituents as defined in the specification; X is -(CR8R8')n-D-(CR8R8')m-; D is a bond, -NR9-, -0-, -S-, -S(=0)- or -S(=0)2-; and pharmaceutically acceptable salts and prodrugs thereof, have utility as HIV antivirals.
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Page/Page column 80-81
(2008/06/13)
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