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We described the preparation of methoxy-substitued BPPM ((2S,4S)-N-(tert-butoxycarbonyl)-4-(diphenylphosphino)-2-<(diphenylphosphino)-methyl>pyrrolidine) analogues for highly effective asymmetric hydrogenation of (Z)-acetamidocinnamic acid. o-Methoxy-BPPM-Rh+ was very high optical yield (98percent enantiomeric excess (ee), (R)) and p-methoxy-BPPM-Rh+ was very actively catalytic (/=104).On the bases of these result and our respectively control concept, we developed a highly effective chiral ligand (5) for asymmetric synthesis of N-acetylphenylalanine.

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Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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The present invention relates to therapeutic diazobicyclo pyridines and their use in the treatment of arthritis, rheumatoid arthritis, psoriatic arthritis or osteoarthritis, organ transplant, acute transplant or heterograft and homograft rejection, ischemic and reperfusion injury, transplantation tolerance induction, multiple sclerosis, inflammatory bowel disease, ulcerative colitis, Crohn”s disease, lupus, graft vs. host diseases, T -cell mediated hypersensitivity diseases, contact hypersensitivity, delayed-type hypersensitivity, gluten-sensitive enteropathy, Type 1 diabetes, psoriasis, contact dermatitis, Hashimoto”s thyroiditis, Sjogren”s syndrome, autoimmune hyperthyroidism,Graves” Disease, Addison”s disease, autoimmune polyglandular disease, autoimmune alopecia, pernicious anemia, vitiligo, autoimmune hypopituatarism, Guillain-Barre syndrome, autoimmune diseases, glomerulonephritis, serum sickness, uticaria, respiratory allergies, asthma, hayfever, allergic rhinitis, skin allergies, scleracielma, mycosis fungoides, acute inflammatory responses, acute respiratory distress syndrome, dermatomyositis, alopecia areata, chronic actinic dermatitis, eczema, Behcet”s disease, Pustulosis palmoplanteris, Pyoderma gangrenum, Sezary”s syndrome, atopic dermatitis, systemic schlerosis, morphea, Type II diabetes and cancers where PKC theta or other PKC-family kinases are activated, overexpressed or facilitate tumor growth or survival of tumor cells, T cell leukemia, thymoma, T and B cell lymphoma, colon carcinoma, breast carcinoma and lung carcinoma or provides resistance to chemotherapeutic drugs.

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Barmumycin was isolated from an extract of the marine actinomycete Streptomyces sp. BOSC-022A and found to be cytotoxic against various human tumor cell lines. On the basis of preliminary one- and two-dimensional 1H and 13C NMR spectra, the natural compound was initially assigned the structure of macrolactone-type compound 1, which was later prepared by two different routes. However, major spectroscopic differences between isolated barmumycin and 1 led to revision of the proposed structure as E-16. On the basis of the synthesis of this new compound, and subsequent spectroscopic comparison of it to an authentic sample of barmumycin, the structure of the natural compound was indeed confirmed as that of E-16.

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Metal catalyst and ligand design,
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The invention relates to novel chimeric antibiotics of formula (I) wherein R1 represents OH, OPO3H2 or OCOR5; R2 represents H, OH or OPO3H2; R3 represents H or halogen; R4 is H, (C1-C3) alkyl, or cycloalkyl; R5 represents piperidin-4-yl or R5 is the residue of a naturally occurring amino acid, of the enantiomer of a naturally occurring amino acid or of dimethylaminoglycine; n is O or 1; and to salts (in particular pharmaceutically acceptable salts) of compounds of formula (I). These chimeric compounds are useful in the manufacture of medicaments for the treatment of infections (e.g. bacterial infections).

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Metal catalyst and ligand design,
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The invention concerns a compound of the formula (I): wherein, for example:T is of the formula (IA), (IB), or (IC); R1 is of the formula ?NHC(=O)Rb wherein Rb is (1-4C)alkyl;R2 and R3 are hydrogen or fluoro;>A?B? is >C=CH? (but not when T is (IA)) or >CH?CH2?;wherein when T is of the formula (IA) or (IB);R6 is, for example, (1-4C)alkyl; R5 is hydrogen, R10CO?, R10SO2? or R10CS? wherein R10 is, for example, optionally substituted phenyl, or (1-10C)alkyl,or when T is of the formula (IA), (IB); or (IC):R5 and R6 are linked to give a 5- or 6-membered ring which is fused to the ring shown in (IA), (IB), or (IC) so as to give an optionally substituted bicyclic ring;and pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them, and their use as antibacterial agents.

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Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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Four isomers of the monomer of peptide nucleic acid (PNA) were derived from (2S,4R)-4-hydroxyproline; they had different stereochemistries at the C 2 and C4 positions in the pyrrolidine ring. These different backbone conformations corresponding to four different stereochemistries were realized through a combination of inversions at the C2 and the C4 positions in pyrrolidine ring. The obtained backbone frameworks were reacted with N-benzoyl thymine to give the corresponding PNA monomers. Spectroscopic comparison of the resultant monomers confirmed their stereochemistries.

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Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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A series of non-basic building blocks was synthesized and introduced to the C7 position of the quinolone nucleus 7-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid to afford the corresponding fluoroquinolones in 46-85% yield. The antibacterial activity of these new fluoroquinolones was evaluated using a standard broth microdilution technique. The sulfur-containing quinolone, 7-(2-thia-5-azabicyclo[2.2.1]heptan-5-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid exhibited a superior antibacterial activity against quinolone-susceptible and multidrug-resistant strains in comparison with the clinically used fluoroquinolones ciprofloxacin and vancomycin, especially to the Streptococcus pneumonia and multidrug-resistant S. pneumonia clinical isolates. Crown Copyright

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Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

Extracurricular laboratory:new discovery of Boc-Hyp-OL

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Chiral phosphinopyrrolidine compounds and their use for asymmetric synthesis of optically active compounds

New chiral phosphinopyrrolidine compounds of the general formula: STR1 wherein R1 is hydrogen or –COA1, –COOA2, –CONHA3, –SO2 A4 or –PO(A5)2, A1, A2, A3, A4 and A5 each represents independently alkyl or aryl, R2 is phenyl, di(lower-alkyl)aminophenyl, lower-alkoxyphenyl or 3,5-dimethyl-4-methoxyphenyl, and R3 is phenyl, lower-alkylphenyl, di(lower-alkyl)aminophenyl, lower-alkoxyphenyl or 3,5-dimethyl-4-methoxyphenyl, with the proviso that R2 and R3 may not simultaneously by phenyl, p-di(lower-alkyl)-aminophenyl or p-lower-alkoxyphenyl, as well as the use of these compounds as ligand for a metal complex catalyst for asymmetric synthesis of optically active compounds. The new chiral phosphinopyrrolidine compounds are useful ligands which attain both of high optical yield and high reaction efficiency in catalytic asymmetric reduction.

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Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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HDAC INHIBITORS AND USES THEREOF

Inhibitors of histone deacetylase, including compounds having a diazabicyclo[2.2.1]heptan-2-yl moiety are described together with methods for treating various disorders with such compounds

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Reference£º
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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CATALYSTS

Catalysts suitable for asymmetric hydrogenation reactions is described comprising the reaction product of a group (8) transition metal compound a chiral phosphine and a chiral diamine of formula (1) in which R1, R 2 R 3 or R 4 are independently hydrogen, a saturated or unsaturated alkyl, or cycloalkyl group, an aryl group, a urethane or sulphonyl group and R 5 , R 6 , R 7 or R8 are independently hydrogen, a saturated or unsaturated alkyl or cycloalkyl group, or an aryl group, at least one of R1, R2 , R3 or R 4 is hydrogen and A is a linking group comprising one or two substituted or unsubstituted carbon atoms.

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Reference£º
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI