摘要:
A process of preparing symmetric C.sub.40 -carotenoids by reacting a C.sub.15 -triphenylphosphonium salt of the formula ##STR1## and a 2,5-bis(1,1-dialkoxy-2-propyl)-2,5-dihydrofuran to form a reaction product containing a diacetyl and a triphenylphosphonium salt, adding a strong base to the reaction product to convert the triphenylphosphonium salt to a carbenium ion, hydrolyzing the diacetyl to a dialdehyde, subjecting the dialdehyde and the carbenium ion to a Wittig reaction to prepare a Wittig reaction product, and converting the Wittig reaction product to the C.sub.40 -carotenoid by acid treatment.
摘要:
Vitamin A alcohol and its lower alkanoic esters are prepared by desulphonation of corresponding sulphones with a solid potassium alcoholate of a primary or secondary lower alcohol at 10.degree. to 50.degree. C. in an anhydrous liquid hydrocarbon.
摘要:
A widely applicable process for the manufacture of carotenoids by a Wittig reaction comprises carrying out the Wittig reaction in a polar reaction medium in a manner such that neither the reactants nor the thus-manufactured carotenoid are significantly dissolved in the reaction medium. An especially suitable reaction medium is a polar, toxicologically harmless solvent which remains monophasic on the addition of water in an amount up to about 30 vol. % and which permits the triarylphosphine oxide which is formed to dissolve well. Lower alcohols and acetone, as sole solvents or as mixtures with one another and/or with water, are especially suitable as the polar reaction medium. This process permits the use of much more concentrated reaction mixtures, simplifies the regeneration of the solvent and generally the reaction procedure, and avoids toxicologically objectionable solvents such as halogenated hydrocarbons.
摘要:
The present invention relates to novel intermediates for the preparation of vitamin A and carotenoids corresponding to the formula (II): ##STR1## in which A represents a hydrogen or an alkyl, alkenyl or alkoxy group containing 1 to 4 carbon atoms, and X represents a carbon atom, and to a process for their preparation and their use, and further relates to compounds for preparing intermediates of formula (II) corresponding to the formula (III): ##STR2## in which R represents a hydrogen atom, an alkyl group having 1 to 10 carbon atoms, an alkenyl group having 2 to 10 carbon atoms, an alkylcarbonyl, alkenylcarbonyl, alkoxyalkyl or alkoxyalkenyl group in which the alkyl groups have 1 to 10 carbon atoms and the alkenyl groups have 2 to 10 carbon atoms, each of said groups being linear or branched and each being substituted or unsubstituted.
摘要:
The present invention relates to a new method of condensing polyenic compounds wherein a compound having the formula III ##STR1## is condensed with a compound having the formula IV ##STR2## under the influence of a Lewis acid or a protic acid. R.sub.1 through R.sub.7 represent alkyl or alkenyl groups, A' is preferably chlorine, B is preferably a hydroxyl group, and n' is 0 to 10. The invention also relates to novel intermediates for use in the preparation of Vitamins A and E produced by means of the new method.
摘要:
An improved process for the preparation of polyenes by the Julia reaction comprises carrying out the allylation of the anion of an allyl aryl sulfone generated a strong base, and the elimination of arylsulfinic acid to form a double bond in the same inert polar solvent which is immiscible with water, preferably in a ketone of the formula IR.sup.1 --CO--R.sup.2 (I)where R.sup.1 and R.sup.2 are each straight-chain or branched alkyl of 2 to 4 carbons, or R.sup.1 and R.sup.2 together are tetramethylene or pentamethylene. The process is particularly important for the preparation of vitamin A derivatives. In the preparation of vitamin A aldehyde, for example, it is advantageous to use the same alkali metal alcoholate as strong base in both stages so that the conversion can be carried out as one-pot reaction.
摘要:
The invention provides a process for producing vitamin A or its carboxylic acid ester by treating inexpensive and readily available industrial starting materials with potassium hydroxide which is widely employed industrially and is inexpensive.
摘要:
Retinoid-like activity is exhibited by compounds of the formula ##STR1## where n is 0-5 and A is H, lower alkyl, or --COOH or ester or amide thereof, --CH.sub.2 OH or an ether or ester derivative, or --CHO or an acetal derivative, or a pharmaceutically acceptable salt.
摘要:
This invention discloses (20R)-2α-methyl-19,26,27-trinor-vitamin D analogs, and specifically (20R)-2α-methyl-19,26,27-trinor-1α,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits transcription activity as well as pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also shows very low activity in vivo on bone calcium mobilization and intestinal calcium transport activity compared to the native hormone 1α,25-dihydroxyvitamin D3, and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.