- Preparation process for 3-methyl-5-methoxybenzenesulfonyl chloride
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The invention discloses a preparation process for 3-methyl-5-methoxybenzenesulfonyl chloride. The process comprises the following steps: 3,5-dibromotoluene is used as an initial raw material, the 3,5-dibromotoluene is subjected to a boronic acidification reaction, thus 3-methyl-5-bromophenylboronic acid is obtained, the 3-methyl-5-bromophenylboronic acid is subjected to an oxidation reaction, thus 3-methyl-5-bromophenol is obtained, the 3-methyl-5-bromophenol is subjected to a substitution reaction, thus 3-methyl-5-bromoanisoles is obtained, the 3-methyl-5-bromoanisoles is subjected to sulfonation, thus 3-methyl-5-methoxybenzenesulfonate is obtained, the 3-methyl-5-methoxybenzenesulfonate is subjected to a substitution reaction, and therefore the objective compound 3-methyl-5-methoxybenzenesulfonyl chloride is obtained. According to the above route, the raw materials are easy to obtain, post-treatment is simple, convenient and easy to implement, a yield is relatively high, and the process has relatively-good application value.
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- HETEROCYCLIC CARBOXYLIC ACIDS AS ACTIVATORS OF SOLUBLE GUANYLATE CYCLASE
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The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R5, R6, R7, R8, R9, B, V, W, X, Y, Z and m are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
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Paragraph 0324-0325
(2016/02/18)
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- ALKOXY PYRAZOLES AS SOLUBLE GUANYLATE CYCLASE ACTIVATORS
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The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein. The inventi
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Paragraph 0297; 0313
(2014/03/25)
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- 17BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 INHIBITORS FOR THE TREATMENT OF HORMONE-RELATED DISEASES
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The invention relates to the use of non-steroidal 17beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment and prophylaxis of hormone-dependent, particularly estrogen-dependent, diseases.The invention further relates to suitable inhibitors and to a method for the production thereof.
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Page/Page column 13-14
(2010/08/18)
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- NOVEL HIV REVERSE TRANSCRIPTASE INHIBITORS
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The invention is related to compounds of Formula (I) or a pharmaceutically acceptable salt, solvate, ester, and/ or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.
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Page/Page column 423
(2009/03/07)
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- RENIN INHIBITORS
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Disclosed are compounds of Formula (I) wherein the R, R1, R2, R3, X, Y, A, Q, E, and G are defined herein. These compounds bind to aspartic proteases to inhibit their activity and are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also disclosed are methods of use of the compounds of Formula I for ameliorating or treating aspartic protease related disorders in a subject in need thereof.
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Page/Page column 138
(2008/12/04)
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- RENIN INHIBITORS
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Described are compounds which bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also described are methods of use of the compounds described herein in ameliorating or treating aspartic protease related disorders in a subject in need thereof.
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Page/Page column 118
(2008/12/04)
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- 2-PHENYL INDENE DERIVATIVES USEFUL AS ESTROGEN RECEPTOR LIGANDS
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The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity. Formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and R12 are as defined in the specification, and wherein either the bond between the C1and C2 carbon atoms is a double bond or the bond between the C2 and C3 carbon atoms is a double bond, R2 being absent when the bond between the C1 and C2 carbon atoms is a double bond.
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Page/Page column 32-33
(2008/06/13)
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- SHIP 1 MODULATOR COMPOUNDS
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The present invention provides the use of pelorol analogs of Formula, ( I ) and pharmaceutical compositions thereof as modulators of SHIP 1 activity. A compound or a pharmaceutical composition of the present invention may be used for the treatment or prop
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Page/Page column 51-52
(2008/06/13)
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- A short and concise asymmetric synthesis of hamigeran B
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The interesting biological properties of the hamigerans wherein hamigeran B is a potent antiviral agent with low cytotoxicity to host cells make these deceptively simple looking structures challenging synthetic targets. A strategy to hamigeran B evolved wherein the three contiguous stereocenters are established ultimately from a Pd catalyzed asymmetric allylic alkylation (AAA). The latter involves an asymmetric allylation of a non-stabilized ketone enolate in 77% yield and 93% ee. By using this process, (S)-5-allyl-2-isopropyl-5- methyl-1-trifluoromethanesulfonyloxycyclopentene becomes available in four steps from 2-methylcyclopentanone. Introduction of the aryl unit by cross-coupling proceeded intermolecularly but failed intramolecularly. On the other hand, reductive removal of the triflate permitted a Heck reaction to effect intramolecular introduction of the aryl ring. The unusual conformational properties of this molecular architecture are revealed by the regioselectivity of the β-hydrogen elimination in the Heck reaction and the diastereoselectivity of the reduction establishing the stereochemistry of the carbon bearing the isopropyl group. The successful route consists of 15 steps from 2-methylcyclopentanone and dimethylorcinol illustrating the efficiency of the route based upon the Pd AAA.
- Trost, Barry M.,Pissot-Soldermann, Carole,Chen, Irwin
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p. 951 - 959
(2007/10/03)
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- 2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1
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A series of 2-amino-5-arylthiobenzonitriles (1) was found to be active against HIV-1. Structural modifications led to the sulfoxides (2) and sulfones (3). The sulfoxides generally showed antiviral activity against HIV-1 similar to that of 1. The sulfones, however, were the most potent series of analogues, a number having activity against HIV-1 in the nanomolar range. Structural-activity relationship (SAR) studies suggested that a meta substituent, particularly a meta methyl substituent, invariably increased antiviral activities. However, optimal antiviral activities were manifested by compounds where both meta groups in the arylsulfonyl moiety were substituted and one of the substituents was a methyl group. Such a disubstitution led to compounds 3v, 3w, 3x, and 3y having IC50 values against HIV-1 in the low nanomolar range. When gauged for their broad-spectrum antiviral activity against key non-nucleoside reverse transcriptase inhibitor (NNRTI) related mutants, all the di-meta-substituted sulfones 3u-z and the 2-naphthyl analogue 3ee generally showed single-digit nanomolar activity against the V106A and P236L strains and submicromolar to low nanomolar activity against strains E138K, V108I, and Y188C. However, they showed a lack of activity against the K103N and Y181C mutant viruses. The elucidation of the X-ray crystal structure of the complex of 3v (739W94) in HIV-1 reverse transcriptase showed an overlap in the binding domain when compared with the complex of nevirapine in HIV-1 reverse transcriptase. The X-ray structure allowed for the rationalization of SAR data and potencies of the compounds against the mutants.
- Chan,Hong,Hunter III,Orr,Cowan,Sherman,Sparks,Reitter,Andrews III,Hazen,St. Clair,Boone,Ferris,Creech,Roberts,Short,Weaver,Ott,Ren,Hopkins,Stuart,Stammers
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p. 1866 - 1882
(2007/10/03)
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- Sulfinyl and sulfonyl substituted 3-benzazepines
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Sulfinyl and sulfonyl substituted 3-benzazepine compounds are useful in treating gastrointestinal motility disorders. A particular compound of this invention is 8-hydroxy-7-methylsulfonyl-2,3,4,5-tetrahydro-1H-3-benzazepine.
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- Naturally Occurring Dibenzofurans. Part 5. Synthesis of Melacarpic Acid
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The total synthesis of the lichen dibenzofuran melacarpic acid (5) was achieved by intramolecular Ullman coupling of methyl 5-bromo-4-(2-bromo-5-methoxy-3-methylphenoxy)-6-heptyl-2-methoxybenzoate (48) or methyl 6-heptyl-5-iodo-4-(2-iodo-5-methoxy-3-methyl-4-nitrophenoxy)-2-methoxybenzoate (46) followed by appropriate transformations.
- Carvalho, Christopher F.,Sargent, Melvyn V.
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p. 1613 - 1620
(2007/10/02)
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