摘要:
The present invention provides convergent processes for preparing (-)-beta-elemene, (-)-beta-elemenal, (-)-beta-elemenol, and (-)-beta-elemene fluoride and analogues thereof. Also provided are intermediates useful for preparing (-)-beta-elemene. The present invention further provides novel compositions based on analogues of (-)-beta-elemene, (-)-beta-elemenal, (-)-beta-elemenol, (-)-beta-elemene fluoride and methods for the treatment of cancer, such as brain tumor, lung cancer, breast cancer, prostate cancer, ovarian cancer, colorectal cancer, gastric intestional cancer, and stomach cancer. The inventors propose a combination therapy using 1) one or more of the following anti-cancer agents: including, but not limited to, Cisplatin, 5-FU, Taxol, Taxol derivatives, and any anti-cancer agent, and 2) one or more of the following (-)-beta-elemene and its analogs, including (-)-beta-elemene, (-)-beta-elemenol, (-)-beta-elemenol, (-)-beta-elemene fluoride, and their analogs, and (-)-beta-elemene's intermediate in its chemical synthesis, for the treatment of cancer, especially for the treatment of brain tumor, lung cancer, ovarian cancer, bladder cancer, cervical cancer,. colon cancer, breast cancer, and prostate cancer.
摘要:
The present invention pertains generally to compositions comprising organocatalysts that facilitate stereo-selective reactions and the method of their synthesis and use. Particularly, the invention relates to metal-free organocatalysts for facilitation of stereo-selective reactions, and the method of their synthesis and use. These compounds have the structure of the Formulas (I) and (II). Where X is independently selected from CH 2 , N-R a , O, S or C=O; Y is CH 2 , N-R a , O, S or C=O, with the proviso that at least one of X or Y is CH 2 , and preferably both of X and Y are CH 2 ; R a is H, an optionally substituted C 1 -C 12 alkyl, preferably an optionally substituted C 1 -C 6 alkyl including a C 3 -C 6 cyclic alkyl group, or an optionally substituted aryl group, preferably an optionally substituted phenyl group; R b is H, an optionally substituted C 1 -C 12 alkyl, preferably an optionally substituted C 1 -C 6 acyclic or a a C 3 -C 6 cyclic alkyl group, CHO, N(Me)O, CO(S)R a or the group of Formula (III). Where R c and R d are each independently H, F, C1, an optionally substituted C 1- C 20 alkyl, preferably an optionally substituted C 1 -C 12 alkyl, more preferably a C 1 -C 6 alkyl, and an optionally substituted aryl group, or together R c and R d form an optionally substituted carbocyclic or optionally substituted heterocyclic ring; R 1 is OH, OR, NR'R", NHC(=O)R, NHSO 2 R; R 2 is H, F, C1, an optionally substituted C 1- C 20 alkyl, preferably an optionally substituted C 1 C 6 alkyl, an optionally substituted aryl group or a =O group (which establishes a carbonyl group with the carbon to which =O is attached; R 3 is H, OH, F, C1, Br, I, Cl, an optionally substituted C 1 -C 20 alkyl, alkenyl or alkynyl ("hydrocarbyl") group, preferably an optionally substituted C 1 -C 6 alkyl, or an optionally substituted aryl, such that the carbon to which R 3 is attached has an R or S configuration; R is H, an optionally substituted C 1 -C 20 alkyl, preferably an optionally substituted C 1 -C 6 alkyl, or an optionally substituted aryl group, R' and R" are each independently H, an optionally substituted C 1 -C 20 alkyl group, preferably an optionally substituted C 1 -C 6 alkyl, or an optionally substituted aryl group; or together R' and R" form an optionally substituted heterocyclic, preferably a 4 to 7 membered optionally substituted heterocyclic group or an optionally substituted heteroaryl ring with the nitrogen to which R' and R" are attached; and wherein said compound is free from a metal catalyst.
摘要:
Compounds of formula (I) or (II), wherein R is a substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, aralkyl aralkenyl, or aralkynyl group, that optionally includes at least one heteroatom in its carbon skeleton, and R 1 is a substituted or unsubstituted, branched or straight chain alkyl, alkenyl, or alkynyl group, that contains 1-12 carbon atoms, and there use in therapeutic methods.
摘要:
The invention relates to carbonyl compounds of the general structure (I) where the rest R is hydrogen or an alkyl group with between 1 and 5 carbon atoms, the rests R and R independently of each other are hydrogen or an alkyl group with between 1 and 3 carbon atoms and one of the positions C-1/C-2, C-2/C-3 or C-1/C-6 has a C=C double bond, and the rest R is either hydrogen or, if the C=C double bond is situated in position C-2/C-3, hydrogen or an alkyl group with between 1 and 3 carbon atoms. The above compounds are characterized by interesting fragrance notes of great intensity and are suitable for use as fragrances in, for example, cosmetic preparations, technical products or perfumed spirits.
摘要:
The invention relates to a process for the preparation, in a single step, of substituted 2-cyclopenten-l-ones by reacting a substituted enone with an aldehyde in the presence of a catalytic system. Said catalytic system consists of a metal complex, such as a [Ti(Cl) 3 (alkoxy)], and a co-ingredient, such as a carboxylic acid anhydride or an anhydrous salt.
摘要:
Compositions that include compounds capable of producing a cooling sensory effect such as certain hydroxy-ketones and hydroxy-aldehyde compounds, their cyclic semi-ketals and semiacetals, and other derivatives thereof. The compounds impart a refreshing and cooling sensation of long duration and high potency, and thus are useful in a variety of formulations, including consumer products such as mouth formulations, food and beverage products, tobacco and smoking articles, fragrances, toiletries, oinments, and the like.
摘要:
Compositions that include compounds capable of producing a cooling sensory effect such as certain hydroxy-ketones and hydroxy-aldehyde compounds, their cyclic semi-ketals and semiacetals, and other derivatives thereof. The compounds impart a refreshing and cooling sensation of long duration and high potency, and thus are useful in a variety of formulations, including consumer products such as mouth formulations, food and beverage products, tobacco and smoking articles, fragrances, toiletries, oinments, and the like.
摘要:
A compound of formula (I) or (II): wherein A is hydrogen or CR R ; Y and Z are each, independently, hydrogen or a halogen; X is -NR R , or R ; R is hydrogen, or a substituted or unsubstituted alkyl or alkenyl group containing 1-4 carbon atoms; when X is -NR R , R is a substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, aralkyl aralkenyl, or aralkynyl group, that optionally includes at least one heteroatom in its carbon skeleton and contains 1-12 carbon atoms; when X is R , R is an unsubstituted alkyl, alkenyl or alkynyl group, or a substituted or unsubstituted aryl, aralkyl aralkenyl, or aralkynyl group, that optionally includes at least one heteroatom in its carbon skeleton and contains 1-12 carbon atoms; R is a substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, aralkyl aralkenyl, or aralkynyl group, that optionally includes at least one heteroatom in its carbon skeleton and contains 1-12 carbon atoms; R is hydrogen, a substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, aralkyl aralkenyl, or aralkynyl group, that optionally includes at least one heteroatom in its carbon skeleton and contains 1-12 carbon atoms, -COOR , or -COR ; R is hydrogen, or a substituted or unsubstituted alkyl or alkenyl group containing 1-5 carbon atoms; R is an unsubstituted alkyl, alkenyl, or alkynyl group, that contains 1-4 carbon atoms; and, R is an unsubstituted or halo-substituted alkyl, aryl, or aralkyl group, that contains 1-12 carbon atoms.
摘要翻译:式(I)或(II)的化合物:其中A是氢或CR 1 R 2; Y和Z各自独立地为氢或卤素; X是-NR 4 R 5或R 7; R 1是氢或含有1-4个碳原子的取代或未取代的烷基或链烯基; 当X是-NR 4 R 5时,R 2是取代或未取代的烷基,烯基,炔基,芳基,芳烷基芳烯基或芳炔基,其任选地在其碳骨架中包括至少一个杂原子,并且含有 1-12个碳原子; 当X是R 7时,R 2是未取代的烷基,烯基或炔基,或取代或未取代的芳基,芳烷基芳烯基或芳炔基,其任选地在其碳骨架中包含至少一个杂原子,并含有1 -12个碳原子; R 3是任选地在其碳骨架中包含至少一个杂原子并且含有1-12个碳原子的取代或未取代的烷基,烯基,炔基,芳基,芳烷基芳烯基或芳炔基, R 4是氢,取代或未取代的烷基,烯基,炔基,芳基,芳烷基芳烯基或芳炔基,其任选地在其碳骨架中包含至少一个杂原子并含有1-12个碳原子,-COOR 8 或-COR 8; R 5是氢或含有1-5个碳原子的取代或未取代的烷基或链烯基; R 7是含有1-4个碳原子的未取代的烷基,烯基或炔基; 并且R 8是含有1-12个碳原子的未取代或卤素取代的烷基,芳基或芳烷基。