C07C2603/66

Synthesis of Tetracyclines and intermediates thereto

The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for substituents at positions 4a, 5, 5a, and 12a of the tetracycline ring system.

Cyclopropanation

A method of preparing a cyclopropane ring-bearing compound of the formula I ##STR00001##
in which R.sup.1 and R.sup.2 are independently selected from C.sub.1-C.sub.10 alkyl, optionally substituted, or R.sup.1 and R.sup.2, together with the bonds linking them to the cyclopropane ring, form a monocyclic or bicyclic ring system, which may comprise at least one hetero-atom, comprising the reaction of a compound of formula II
R.sup.1CHCHR.sup.2II
in which R.sup.1 and R.sup.2 have the significances hereinabove defined, with a compound of formula III
XCH.sub.2YIII
in which X is a nucleofuge selected from halides and pseudohalides and Y is an electrofuge selected from boranes and borates, in the presence of a metal catalyst complex selected from those useful for catalytic cyclopropanation and those useful for catalyzing Heck coupling. The method provides a particularly easy and non-hazardous method of cyclopropanation.

Method for the synthesis of khusimone

A novel method for synthesis of khusimone, by bringing zizanal into contact with an oxidizing reagent in the presence of a base and an organic solvent.

Organic compound and organic light emitting device using the same

The present invention provides an organic light emitting device comprising a first electrode, at least one organic layer and a second electrode, laminated successively, in which at least one layer of the organic layer has a polycyclic aromatic hydrocarbon as a core and comprises at least one of a derivative in which a substituted or unsubstituted C.sub.2-30 cycloalkane, or a substituted or unsubstituted C.sub.5-50 polycycloalkane is directly fused to the core or fused to a substituent of the core; and a new organic compound usable in the organic light emitting device. Furthermore, the present invention provides a charge carrier extracting, injecting or transporting material which has a polycyclic aromatic hydrocarbon as a core and comprises a derivative in which a substituted or unsubstituted C.sub.2-30 cycloalkane, or a substituted or unsubstituted C.sub.5-50 polycycloalkane is directly fused to the core or fused to a substituent of the core.

Compositions Containing Tri-Cyclopentadiene and Processes for Making Same

Compositions containing tri-cyclopentadiene and processes for making same. In some embodiments, the composition can include 1 wt % to 6 wt % of TCPD-7; 5 wt % to 25 wt % of TCPD-3; 15 wt % to 30 wt % of TCPD-5; and 55 wt % to 75 wt % of TCPD-1, where all wt % values are based on the combined weight of TCPD-7, TCPD-3, TCPD-5, and TCPD-1 in the composition. In some embodiments, the composition can further include di-cyclopentadiene. In other embodiments, the composition can further include di-cyclopentadiene, tetra-cyclopentadiene, and optionally one or more oligomers heavier than tetra-cyclopentadiene. In some embodiments, the composition can be made via a continuous process.

5,5-dimethyl-2-propyl-hexahydro-2,4a-methano-naphthalen-1-one as a fragrance agent
09556400 · 2017-01-31 · ·

The invention relates to a compound of general formula (I) shown hereafter: ##STR00001##
as well as a composition comprising at least said compound of general formula (I), and its uses in perfumery.

N-SUBSTITUTED BENZAMIDES AND METHODS OF USE THEREOF

The invention provides novel compounds having the general formula:

##STR00001##

and pharmaceutically acceptable salts thereof, wherein the variables R.sup.A, subscript n, ring A, X.sup.2, L, subscript m, X.sup.1, B, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.N have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.

Oxidation of santalene to santalol

The invention relates to a process for the oxidation of santalene to santalol. The starting material is in particular a mixture comprising alpha-santalene, beta-santalene, epi-beta-santalene, trans-alpha-bergamotene and beta-bisabolene. The oxidation of the santalenes occurs via an intermediate chloro-santalene compound. Substitution of the chloro-substituent by acetate yielded the mixture of the corresponding santalyl acetates, which were hydrolyzed to yield the corresponding mixture of santalols.

BRIDGED TRICYCLIC GABA DERIVATIVES AS CALCIUM CHANNEL MODULATORS, METHODS OF MAKING AND METHODS OF USING THEREOF

This invention discloses bridged tricyclic -aminobutyric acid (GABA) derivatives targeting the 2 subunit of voltage-gated calcium channels. These compounds exhibit enhanced binding affinity and improved pharmacological profiles. They aim to overcome limitations of current 2 ligands like gabapentin and pregabalin. The new derivatives show potential for treating neuropathic pain, epilepsy, and related disorders.