CAS: 1321-23-9; Chloroxylenol

上下游产品

二甲酚 2,3-Dimethylphenol 526-75-0

📜二甲酚置于磺酰氯体系中,用 乙醚,二氯甲烷 用作溶剂,化学反应 0.5H,以75%的收率获得氯二甲酚(Pcmx)
参考文献:Benzoxazole Derivatives As Novel 5-Ht3 Receptor Partial Agonists In The Gut
标题:Benzoxazole Derivatives As Novel 5-Ht3 Receptor Partial Agonists In The Gut
摘要:A Series Of Benzoxazoles With A Nitrogen-Containing Heterocyclic Substituent At The 2-Position Was Prepared And Evaluated For 5-Ht3 Partial Agonist Activity On Isolated Guinea Pig Ileum. The Nature Of The Substituent At The 5-Position Of The Benzoxazole Ring Affected The Potency For The 5-Ht3 Receptor,And The 5-Chloro Derivatives Showed Increased Potency And Lowered Intrinsic Activity. 5-Chloro-7-Methyl-2-(4-Methyl-1-Homopiperazinyl)Benzoxazole (6V) Exhibited A High Binding Affinity In The Same Range As That Of The 5-Ht3 Antagonist Granisetron,And Its Intrinsic Activity Was 12% Of That Of 5-Ht. Compound 6V Inhibited 5-Ht-Evoked Diarrhea But Did Not Prolong The Transition Time Of Glass Beads In The Normal Distal Colon Even At A Dose Of 100 Times The Ed50 For Diarrhea Inhibition In Mice. Compounds Of This Type Are Expected To Be Effective For The Treatment Of Irritable Bowel Syndrome Without The Side Effect Of Constipation.
Doi:10.1021/jm9801004

专利信息

专利号:US-12221452-B2
优先权日:2017-10-04
标题:Synthesis of cantharidin
发明人：DAVIDSON MATTHEW GENE; EKLOV BRIAN MATTHEW; WUTS PETER; LOERTSCHER BRAD MELVIN; SCHOW STEVEN R
权利人:VERRICA PHARMACEUTICALS INC
摘要:The invention provides synthetic methods for the preparation of cantharidin and analogs thereof. In one aspect, the invention provides an improved Diels-Alder cycloaddition to generate a key intermediate en route to cantharidin and analogs thereof. In certain embodiments, the new Diels-Alder reaction involves reacting Compound (2) in the presence of furan, and in the absence of acid or increased pressure, in an aprotic polar solvent with slight warming, to yield Compound (1) in favorable yield and exo-endo ratio. In another aspect, the invention also provides a new Diels-Alder reaction between compounds of Formula (III) and furan to yield compounds of Formula (IV), which can then be transformed into cantharidin or analogs thereof. In yet another aspect, the invention describes a new palladium-mediated carbonylation providing another key intermediate en route to cantharidin and analogs thereof. In addition to synthetic methods, present invention also provides compounds (i.e., intermediates) useful in the synthesis of cantharidin and analogs thereof. Compounds provided herein may have biological activity, and therefore may be used in the treatment of diseases or conditions (e.g., infectious diseases and skin conditions).

专利号:US-11155562-B2
优先权日:2014-06-30
标 题 :Synthesis of halichondrin analogs and uses thereof
发明人：KISHI YOSHITO; UEDA ATSUSHI; YAMAMOTO AKIHIKO; KATO DAISUKE
权利人:HARVARD COLLEGE
摘要:The present invention provides halichondrin analogs, such as compounds of Formula (I). The compounds may bind to microtubule sites, thereby inhibiting microtubule dynamics. Also provided are methods of synthesis, pharmaceutical compositions, kits, methods of treatment, and uses that involve the compounds for treatment of a proliferative disease (e.g., cancer). Compounds of the present invention are particularly useful for the treatment of metastatic breast cancer, non-small cell lung cancer, prostate cancer, and sarcoma. The included methods of synthesis are useful for the preparation of compounds of Formula (I)-(III) along with naturally occurring halicondrins (e.g., halichondrin B & C, norhalichondrin A, B, & C, and homohalichondrin A, B, & C). Also included are methods for interconverting between the halichondrins, norhalichondrins, and homohalichondrins and their unnatural epimers at the C38 ketal stereocenter through the use of an acid-mediated equilibration.

专利号:US-9982005-B2
优先权日:2013-04-04
标 题 :Macrolides and methods of their preparation and use
发明人：MYERS ANDREW G; SEIPLE IAN BASS; ZHANG ZIYANG
权利人:HARVARD COLLEGE
摘要:Provided herein are methods of preparing macrolides by the coupling of an eastern and western half, followed by macrocyclization, to provide macrolides, including both known and novel macrolides. Intermediates in the synthesis of macrolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using the inventive macrolides are also provided. A general diastereoselective aldol methodology used in the synthesis of the western half is further provided.

专利号:US-2014378538-A1
优先权日:2011-12-14
标 题:Methods of responding to a biothreat
发明人：BANCEL STEPHANE
权利人:MODERMA THERAPEUTICS INC
摘要:The present disclosure provides for devices, in particular mobile devices, which may be used in the synthesis of modified nucleic acid molecules, in particular modified mRNA molecules. The device for making the modified nucleosides, modified nucleotides and modified nucleic acids (e.g., mRNA) disclosed herein may be mobile devices comprising at least one sample block for insertion of one or more sample vessels, a device base with electronic control units for the sample block, a voltage supply, and one or more reagent(s) for the synthesis of at least one nucleic acid.

专利号:US-2024309142-A1
优先权日:2023-03-17
标题 :Capped block copolymers, their synthesis, manufacture, and methods of use
发明人：MAN VICTOR FUK-PONG; LI XIAOJIN HARRY; CHEN YIQING; PU GANG; HUNT JR CLINTON
权利人:ECOLAB USA INC
摘要:This disclosure relates to capped block copolymers, preferably reverse block copolymers capped with a hydrophobic group. Preferred hydrophobic groups include benzyl groups and silyl groups. In a preferred embodiment, the reverse block copolymer has at least two arms, wherein each arm is capped with a hydrophobic group. The disclosure also provides for the synthesis of the capped block copolymers as well as methods of using the capped block copolymers for defoaming and antifoaming applications.

专利号:US-6193975-B1
优先权日:1996-11-07
标题:Use of potentilla erecta extract in the cosmetic and pharmaceutical field
发明人：BONTE FREDERIC; DUMAS MARC; CHAUDAGNE CATHERINE; MEYBECK ALAIN
权利人:LVMH RECH
摘要:The invention relates to the use of an extract of the plant Potentilla erecta in the field of cosmetics and pharmacy, especially in dermatology. The invention more particularly relates to any application in which it is sought to reinforce the dermo-epidermal junction or to improve hair condition, by the improvement of the synthesis of collagen VII by keratinocytes and/or fibroblasts. In particular, these applications concern toning of the skin, diminishing of wrinkles or hair care. The invention also relates to a novel method of culture of cells, in particular of human fibroblasts or keratinocytes, for promoting the formation of collagen VII.