13737-36-5Relevant academic research and scientific papers
Synthesis of α-Helices Having a Positively Charged Random Coil-Block on Either N- or C-Terminal
Takahashi, Sho,Hibino, Takeshi,Sawada, Seiji
, p. 2467 - 2472 (1988)
To study a charge-induced stabilization of α-helix, α-helical peptides having a positively charged random-coil block on either N- or C-terminal of the helix, and having a strictly defined length, (Ala)20(X)20Phe and (X)20(Ala)20Phe(X=Lys or Orn), were syn
Photocatalytic continuous bromination method
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Paragraph 0060-0061, (2021/04/03)
The invention provides a photocatalytic continuous bromination method. The method comprises the following steps: carrying out a first-stage photocatalytic continuous bromination reaction on a materialcontaining an aromatic substrate with a structural general formula I and a bromination reagent in a first continuous illumination reactor to form a first continuous system; overflowing the obtained first continuous system into a second continuous illumination reactor for a second-stage photocatalytic continuous bromination reaction to form a second continuous system; and purifying the second continuous system, wherein the structural general formula I is shown in the specification, R is selected from any one of carboxyl, ester group, NO2, CN, C1 to C8 alkyl and alkoxy, and R1 is C1 to C8 alkyl; n is 1 or 2; X is N or C, and the bromination reagent is Nbromo succinimide or dibromohydantoin. According to the bromination reagent, the selectivity of a product is improved, so the yield of the product is improved; the photocatalytic continuous bromination reaction of the two stages effectively relieves the reaction heat accumulation, and enhances the yield of the target product.
Preparation method of netarsudil mesylate
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Paragraph 0021, (2021/07/17)
The invention relates to a preparation method of netarsudil mesylate.Netarsudil mesylate is synthesized by utilizing chiral induction, and compared with an existing chiral HPLC method or SFC method, netarsudil mesylate prepared by adopting a chemical synt
Nitroxide derivative of ROCK kinase inhibitor
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Paragraph 0064-0070, (2020/06/17)
The invention provides a small molecular compound of a NO donor. The small molecular compound is characterized in that the small molecular compound is a compound shown represented by structural formula I shown in the description, or a stereoisomer, a geometrical isomer, a tautomer, a racemate, a deuterated isotope derivative, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof; and in the formula I, ring A is a substituted or unsubstituted heteroaromatic ring, X is selected from (CH2)n, n is selected from 0, 1, 2 and 3, R is a substituent group of terminal -O-NO2, R is selected from hydrogen, a hydroxyl group, halogen, an amino group, a cyano group, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkoxy group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted alkynyl group and a substituted or unsubstituted heteroalkyl group, and R and R are respectively and independently selected from hydrogen, a substituted or unsubstituted alkyl group, a substituted or unsubstituted naphthenic base or an amino protecting group, or R and R are connected to form a substituted or unsubstituted cyclic heteroalkyl group. The compound has a high-activity inhibition effect on ROCK kinase.
BIARYL UREA DERIVATIVE OR SALT THEREOF, AND MANUFACTURING AND APPLICATION OF SAME
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Paragraph 0173, (2019/05/10)
The present invention discloses a biaryl urea RORγt inhibitor, and specifically relates to a biaryl urea derivative, as represented by formula I, with an RORγt inhibiting activity, and a preparation process thereof, and a pharmaceutical composition comprising the compound. Further disclosed is use of the compound for treating an RORγt-related disease.
p-bromomethyl phenylacetic acid preparation method
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Paragraph 0018; 0019; 0020; 0021, (2017/07/21)
The present invention provides a p-bromomethyl phenylacetic acid preparation method, which comprises: dissolving p-methyl phenylacetic acid in a high boiling point solvent, wherein the solvent is benzene, chlorobenzene or dichlorobenzene; adding a bromina
Process for the preparation of kinase inhibitors and intermediates thereof
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Page/Page column 33;34, (2017/05/31)
Described are processes for the synthesis of certain compounds, useful for treating diseases, e.g. eye disease, such as glaucoma and ocular hypertension, in a subject.
PROCESS FOR THE PREPARATION OF KINASE INHIBITORS AND INTERMEDIATES THEREOF
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Paragraph 00104, (2017/06/12)
Described are processes for the synthesis of certain compounds, useful for treating diseases, e.g. eye disease, such as glaucoma and ocular hypertension, in a subject.
Preparation method of AR-13324
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Paragraph 0055-0058, (2018/03/28)
The invention relates to a preparation method of AR-13324. According to the invention, a chiral ligand is used for chiral induced synthesis of AR-13324. In comparison with an existing chiral HPLC method or a SFC method, the method of the invention has the
6-Membered heterocyclic compound and use thereof
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Page/Page column 218, (2008/06/13)
A compound represented by the general formula (I) or a salt thereof: [T represents oxygen atom and the like; V represents CH2 and the like; RO1 to RO4 represent hydrogen atom and the like; A represents a linear alkylene group or linear alkenylene group having 2 to 8 carbon atoms and the like; D represents carboxyl group and the like; X represents ethylene group, trimethylene group and the like; E represents —CH(OH)— group and the like; and W represent —U1—(RW1)(RW2)—U2—U3 group (U1 represents a single bond, an alkylene group having 1 to 4 carbon atoms and the like; RW1 and RW2 represent hydrogen atom and the like; U2 represents a single bond, an alkylene group having 1 to 4 carbon atoms and the like; and U3 represent an alkyl group having 1 to 8 carbon atoms and the like), or a residue of a carbon ring or heterocyclic compound], which can be utilized as an active ingredient of medicaments effective for prophylactic and/or therapeutic treatment of skeletal diseases such as osteoporosis and fracture, glaucoma, ulcerative colitis and the like.
