C07D317/44

USE OF AMBROCENIDE ® FOR INTENSIFYING A LILY OF THE VALLEY SCENT
20200239810 · 2020-07-30 ·

The present invention primarily relates to the use of one or more stereoisomers of the compound of formula (I) as described herein for modifying and/or enhancing the olfactory impression of one or more fragrances with a lily of the valley scent. The invention further relates to a new mixture comprising or consisting of one or more stereoisomers of the compound of formula (I) as described herein and two or more stereoisomers of the compound of formula (II) as described herein with a weight ratio of the stereoisomers of the compounds of formula (II) as described herein, fragrance compositions comprising or consisting of a mixture as described herein, perfumed products containing mixtures or fragrance composition as described herein, and a process for modifying and/or enhancing the lily of the valley scent of a compound of formula (II) as described herein, respectively for preparing a perfumed product as described herein.

Synthesis of 2'-Fluoro-6'-Methylene-Carbocyclic Adenosine (FMCA) and 2'-Fluoro-6'Methylene-Carbocyclic Guanosine (FMCG)

The invention provides a new convergent approach for the synthesis of 2-fluoro-6-methylene-carbocyclic adenosine (FMCA) and 2-fluoro-6-methylene-carbocyclic guanosine (FMCG) from a readily available starting material in eight steps. An efficient and practical methodology for stereospecific preparation of a versatile carbocyclic key intermediate, (1S,3R, 4R)-3-tert-butoxy -4-(tert-butoxymethyl)-2-fluoro-5-methylenecyclopentanol (compound 8 of scheme 1A or a) in only six (6) steps is also provided. Prodrugs of these compounds are also prepared.

Synthesis of 2'-Fluoro-6'-Methylene-Carbocyclic Adenosine (FMCA) and 2'-Fluoro-6'Methylene-Carbocyclic Guanosine (FMCG)

The invention provides a new convergent approach for the synthesis of 2-fluoro-6-methylene-carbocyclic adenosine (FMCA) and 2-fluoro-6-methylene-carbocyclic guanosine (FMCG) from a readily available starting material in eight steps. An efficient and practical methodology for stereospecific preparation of a versatile carbocyclic key intermediate, (1S,3R, 4R)-3-tert-butoxy -4-(tert-butoxymethyl)-2-fluoro-5-methylenecyclopentanol (compound 8 of scheme 1A or a) in only six (6) steps is also provided. Prodrugs of these compounds are also prepared.

Synthesis of 2′-fluoro-6′-methylene-carbocyclic adenosine (FMCA) and 2′-fluoro-6′-methylene-carbocyclic guanosine (FMCG)

The invention provides a new convergent approach for the synthesis of 2-fluoro-6-methylene-carbocyclic adenosine (FMCA) and 2-fluoro-6-methylene-carbocyclic guanosine (FMCG) from a readily available starting material in eight steps. An efficient and practical methodology for stereospecific preparation of a versatile carbocyclic key intermediate, (1S,3R,4R)-3-tert-butoxy-4-(tert-butoxymethyl)-2-fluoro-5-methylenecyclopentanol (compound 8 of scheme 1A or a) in only six (6) steps is also provided. Prodrugs of these compounds are also prepared.

Synthesis of 2′-fluoro-6′-methylene-carbocyclic adenosine (FMCA) and 2′-fluoro-6′-methylene-carbocyclic guanosine (FMCG)

The invention provides a new convergent approach for the synthesis of 2-fluoro-6-methylene-carbocyclic adenosine (FMCA) and 2-fluoro-6-methylene-carbocyclic guanosine (FMCG) from a readily available starting material in eight steps. An efficient and practical methodology for stereospecific preparation of a versatile carbocyclic key intermediate, (1S,3R,4R)-3-tert-butoxy-4-(tert-butoxymethyl)-2-fluoro-5-methylenecyclopentanol (compound 8 of scheme 1A or a) in only six (6) steps is also provided. Prodrugs of these compounds are also prepared.

BIOORTHOGONAL LINKERS AND REACTIONS
20240058455 · 2024-02-22 ·

The present disclosure provides bioorthogonal linkers and reagents, including trans-cyclooctene (TCO)- and tetrazine (Tz)-containing compounds. In a general aspect, the present disclosure provides reagents, conjugates, and bioactive molecules containing a trans-cyclooctene (TCO) fragment. Examples of TCO fragments include: Formulae (I) and (II).

##STR00001##

LIPIDS AND COMPOSITIONS FOR THE DELIVERY OF THERAPEUTICS

The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure

##STR00001##

wherein: R.sub.1 and R.sub.2 are each independently for each occurrence optionally substituted C.sub.10-C.sub.30 alkyl, optionally substituted C.sub.10-C.sub.30 alkenyl, optionally substituted C.sub.10-C.sub.30 alkynyl, optionally substituted C.sub.10-C.sub.30 acyl, or -linker-ligand; R.sub.3 is H, optionally substituted C.sub.1-C.sub.10 alkyl, optionally substituted C.sub.2-C.sub.10 alkenyl, optionally substituted C.sub.2-C.sub.10 alkynyl, alkylhetrocycle, alkylphosphate, alkylphosphorothioate, alkylphosphorodithioate, alkylphosphonates, alkylamines, hydroxyalkyls, -aminoalkyls, -(substituted)aminoalkyls, -phosphoalkyls, -thiophosphoalkyls, optionally substituted polyethylene glycol (PEG, mw 100-40K), optionally substituted mPEG (mw 120-40K), heteroaryl, heterocycle, or linker-ligand; and E is C(O)O or OC(O).

LIPIDS AND COMPOSITIONS FOR THE DELIVERY OF THERAPEUTICS

The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure

##STR00001##

wherein: R.sub.1 and R.sub.2 are each independently for each occurrence optionally substituted C.sub.10-C.sub.30 alkyl, optionally substituted C.sub.10-C.sub.30 alkenyl, optionally substituted C.sub.10-C.sub.30 alkynyl, optionally substituted C.sub.10-C.sub.30 acyl, or -linker-ligand; R.sub.3 is H, optionally substituted C.sub.1-C.sub.10 alkyl, optionally substituted C.sub.2-C.sub.10 alkenyl, optionally substituted C.sub.2-C.sub.10 alkynyl, alkylhetrocycle, alkylphosphate, alkylphosphorothioate, alkylphosphorodithioate, alkylphosphonates, alkylamines, hydroxyalkyls, -aminoalkyls, -(substituted)aminoalkyls, -phosphoalkyls, -thiophosphoalkyls, optionally substituted polyethylene glycol (PEG, mw 100-40K), optionally substituted mPEG (mw 120-40K), heteroaryl, heterocycle, or linker-ligand; and E is C(O)O or OC(O).