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The invention provides certain benzoxazine compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, Ra1, Ra2, Rb1, Rb2, Rc, Rd, and Cy are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds of the Formula (I) or pharmaceutically acceptable salts thereof, and methods of using the compounds of the Formula (I) or pharmaceutically acceptable salts thereof or pharmaceutical compositions comprising the same for treating diseases or conditions mediated by RORgammaT.

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Reference:
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The invention relates to a preparation method of a Bruton’s tyrosine kinase (Btk) intermediate (VI). The method comprises the following steps: carrying out benzylamine ring opening on a compound (S)-(+)-5-substituted-2-tetrahydrofurancarboxylic acid to obtain a product, and reacting the product with acyl chloride or acid anhydride to obtain a compound II; reducing the compound II, carrying out salt formation on the reduced compound II by using 1R-(-)-camphorsulfonic acid, and degrading the obtained salt to obtain a compound III; and reducing the compound III, carrying out salt formation on the reduced compound III and AcOH to obtain a compound V, and carrying out Boc addition on the compound V under an alkaline condition to obtain the target compound VI.

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The present invention is directed to a method for the synthesis of a bi-functional complex comprising a molecule part and an identifier oligonucleotide part identifying the molecule part. A part of the synthesis method according to the present invention is preferably conducted in one or more organic solvents when a nascent bi-functional complex comprising an optionally protected tag or oligonucleotide identifier is linked to a solid support, and another part of the synthesis method is preferably conducted under conditions suitable for enzymatic addition of an oligonucleotide tag to a nascent bi-functional complex in solution.

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The present invention is directed to a method for the synthesis of a bi-functional complex comprising a molecule part and an identifier oligonucleotide part identifying the molecule part. A part of the synthesis method according to the present invention is preferably conducted in one or more organic solvents when a nascent bi-functional complex comprising an optionally protected tag or oligonucleotide identifier is linked to a solid support, and another part of the synthesis method is preferably conducted under conditions suitable for enzymatic addition of an oligonucleotide tag to a nascent bi-functional complex in solution.

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A route to analogues of the original structure of sclerophytin A is described. The beta-anomer of dideoxyribosyl nitriles 10a,b (prepared from glutamic acid) was converted into the methyl ketone 11. Addition of a silylated acetylide to 11 in diethyl ether/trimethylamine gave mainly 22a. Alkylation with methallyl halide and ozonolysis gave the ketone 24, which was then converted by hydrogenation and a second ozonolysis into the keto aldehyde 26. A two-step aldol process afforded the desired 3-pyrone 27 in good overall yield. However, several methods for the conversion of this enone 27 into the desired sclerophytin analogue 2 failed.

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In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 21461-84-7, name is (S)-( )-5-Oxo-2-tetrahydrofurancarboxylic Acid, introducing its new discovery. Formula: C5H6O4

Disclosed is an optically active compound represented by the formula: STR1 wherein R1 and R2 are alkyl, alkenyl or alkoxy-alkyl, which may be substituted by halogen, X and U are a direct bond, –O–, –COO– or –OCO–, Y and Z are a direct bond, –COO–, –OCO–, –CH2 O– or –OCH2 –, A1 and A2 are phenylene, cyclohexylene or a phenylene- or cyclohexylene-containing group, p and q are 0 or 1, C* is an asymmetric carbon atom, with the proviso that when Z is a direct bond, q is 0, R2 is alkyl, Y is a direct bond, –OCO– or –OCH2 –. The optically active compound is used as a ferroelectric liquid crystal or an additive to a ferroelectric or non-ferroelectric liquid crystal.

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Herein, we describe the first asymmetric total synthesis of (-)-martinelline ((-)-2) and the second total synthesis of (-)-martinellic acid ((-)-1) by employing a tandem Mukaiyama-Mannich reaction/aminal cyclization as the key step. The Royal Society of Chemistry.

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(Chemical Equation Presented) A small library of chiral, beta3-substituted homopropargyl alcohols and chiral beta3-substituted trimethylsilylhomopropargyl azides were generated starting from natural L-amino acids. The free alkynes and azides were then coupled, using a Huisgen 1,3-dipolar cycloaddition, to provide chiral oligomeric 1,4-disubstituted-1,2,3-triazoles as potential peptidomimetic compounds. The work is an extension to the previous synthesis of racemic, orthogonally protected 1,4-disubstituted-1,2,3-triazoles from the corresponding alpha-substituted propargyl alcohols and alpha-substituted trialkylsilylpropargyl azides.

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A compound of the formula (1) or a pharmaceutically-acceptable salt, or pro-drug thereof; (1) wherein, for example: R4 and R5 together are either -S-C(R6=C(R7)- or -C(R7)=C(R6)-S- ; R6 and R7 are independently selected from hydrogen and halo; A is phenylene or heteroarylene; n is 0, 1 or 2; R1 is halo, cyano or carboxy; R2 is for example methyl; R3 is for example selected from halo(1-4C)alkyl, dihalo(1-4C)alkyl, trifluoromethyl, hydroxy(1-4C)alkyl, dihydroxy(2-4C)alkyl, trihydroxy(3-4C)alkyl, cyano(1-4C)alkyl (optionally substituted on alkyl with hydroxy), (1-4C)alkoxy(1-4C)alkyl, (1-4C)alkoxy(1-4C)alkoxy(1-4C)alkyl, di[(1-4C)alkoxy](1-4C)alkyl, (hydroxy)[(1-4C)alkoxy](1-4C)alkyl; possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity. Processes for the manufacture of compounds and pharmaceutical compositions containing them are described.

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Synthesis of the triol that has been proposed to be the marine natural product sclerophytin F has been completed along with the syntheses of three diastereomers. Comparison of the NMR spectroscopic data for all four compounds to the data reported for the natural product reveals that sclerophytin F is not the 3S diastereomer of sclerophytin A as proposed by Friedrich and Paquette. Re-analysis of the NMR spectroscopic data for known sclerophytin natural products and synthetic analogues leads to the conclusion that sclerophytins E and F are the same compound. This finding has allowed structural reassignment of several other cladiellin natural products.

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Tetrahydrofuran – Wikipedia,
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